U.S. patent number RE34,779 [Application Number 07/946,900] was granted by the patent office on 1994-11-08 for pyrazole derivatives and herbicides containing them.
This patent grant is currently assigned to Nissan Chemical Industries Ltd.. Invention is credited to Takuya Kakuta, Yasuo Kondo, Tsutomu Nawamaki, Eiichi Oya, Koichi Suzuki, Junichi Watanabe, Shigeomi Watanabe.
United States Patent |
RE34,779 |
Oya , et al. |
November 8, 1994 |
**Please see images for:
( Certificate of Correction ) ** |
Pyrazole derivatives and herbicides containing them
Abstract
A pyrazole derivative of the formula I ##STR1## wherein A is
C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2
-C.sub.4 alkynyl; B is hydrogen, C.sub.1 -C.sub.3 alkyl, halogen,
C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1
-C.sub.3 alkylthio, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.2 -C.sub.4
alkylthioalkyl or C.sub.2 -C.sub.4 alkoxycarbonyl; X is C.sub.1
-C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, nitro, cyano,
etc.; Y is --OR.sup.1 (wherein R.sup.1 is C.sub.3 -C.sub.8
cycloalkyl, etc), --O--L--O--R.sup.1 (wherein L is C.sub.1 -C.sub.6
alkylene which may be substituted by C.sub.1 -C.sub.3 alkyl),
--O--L--OH, --O--L--O--L--O--R.sup.2 (wherein R.sup.2 is hydrogen,
C.sub.1 -C.sub.6 alkyl group, etc.), --O--L--R.sup.3 (wherein
R.sup.3 is phenyl which may be substituted by C.sub.1 -C.sub.3
alkyl, etc.), --O--M (wherein M is a 3- to 6-membered alicyclic
group), --O--L--M, --O--L--NR.sup.4 R.sup.5 (wherein each of
R.sup.4 and R.sup.5 is hydrogen or C.sub.1 -C.sub.6 alkyl, or
R.sup.4 and R.sup.5 form a ring together with the adjacent nitrogen
atom), --O--L--COOR.sup.4, --O--CH.dbd.CH--COOR.sup.4, --O--L--CN,
--O--L--C(O)--R.sup.2, --O--L--S(O).sub.n --R.sup.4 (wherein n is
an integer of from 0 to 2), --O--COOR.sup.4, --O--CONR.sup.4
R.sup.5, --OP(O)(OR.sup.4).sub.2, --S(O).sub.n R.sup.1, or
--S(O).sub.n --L--O--R.sup.1 ; Z is halogen, nitro, C.sub.1
-C.sub.3 alkoxy, etc.; V is hydrogen, halogen, C.sub.1 -C.sub.4
alkyl or C.sub.1 -C.sub.4 alkoxy; W is hydrogen, halogen, C.sub.1
-C.sub.4 alkyl, etc.; Q is hydrogen, C.sub.1 -C.sub.6 alkyl which
may be substituted by halogen, . . . --C(O)--R.sup.7 (wherein
R.sup.7 is phenyl which may be substituted), --S(O).sub.2 R.sup.7,
--P(O)(OR.sup.7).sub.2, --L--C(O)--R.sup.7,
--L--C(O)--N(R.sup.8)(R.sup.9) (wherein each of R.sup.8 and R.sup.9
is hydrogenor C.sub.1 -C.sub.6 alkyl), --L--R.sup.10 (wherein
R.sup.10 is phenyl group may be substituted, C.sub.1 -C.sub.6
alkyl, C.sub.1 -C.sub.7 alkoxy, or hydroxyl),
--L--N(R.sup.8)(R.sup.9), --L--OR.sup.11 (wherein R.sup.11 is
hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.1 -C.sub.6 alkenyl),
--L--OC(O)R.sup.12 (wherein R.sup.12 is C.sub.1 -C.sub.6 alkyl or
C.sub.1 -C.sub.6 alkoxy), --L--S(O).sub.n R.sup.11,
--L--SC(O)R.sup.8, ##STR2## (wherein each of L1 and L2 is
methylene, oxygen or sulfur, R.sup.12 is hydrogen or C.sub.1
-C.sub.3 alkyl, and m is 2 or 3); and a salt thereof.
Inventors: |
Oya; Eiichi (Funabashi,
JP), Watanabe; Junichi (Funabashi, JP),
Kondo; Yasuo (Funabashi, JP), Kakuta; Takuya
(Funabashi, JP), Suzuki; Koichi (Shiraoka,
JP), Nawamaki; Tsutomu (Clarence, MO), Watanabe;
Shigeomi (Shiraoka, JP) |
Assignee: |
Nissan Chemical Industries Ltd.
(Tokyo, JP)
|
Family
ID: |
26363753 |
Appl.
No.: |
07/946,900 |
Filed: |
September 18, 1992 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
Issue Date |
|
Reissue of: |
369523 |
Jun 21, 1989 |
04986845 |
Jan 22, 1991 |
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Foreign Application Priority Data
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Jul 15, 1988 [JP] |
|
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63-176758 |
Feb 3, 1989 [JP] |
|
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1-26030 |
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Current U.S.
Class: |
504/282;
548/365.7; 504/196; 504/197; 546/22; 546/211; 548/364.1; 548/119;
548/369.4; 548/367.1; 548/366.7; 544/140; 504/225; 504/248;
548/366.1; 548/366.4 |
Current CPC
Class: |
C07D
231/22 (20130101); C07D 409/12 (20130101); C07C
317/46 (20130101); C07D 231/24 (20130101); A01N
43/56 (20130101); C07F 9/65031 (20130101); C07C
205/37 (20130101); C07D 405/12 (20130101); C07F
9/12 (20130101) |
Current International
Class: |
A01N
43/48 (20060101); A01N 43/56 (20060101); C07D
231/00 (20060101); C07D 231/24 (20060101); A01N
043/56 (); C07D 401/12 (); C07D 413/12 (); C07D
231/20 () |
Field of
Search: |
;548/365.7,366.1,366.4,366.7,367.1,369.4,119 ;504/282,196,197
;546/211,22 |
References Cited
[Referenced By]
U.S. Patent Documents
Foreign Patent Documents
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|
0203428 |
|
Dec 1986 |
|
EP |
|
0282944 |
|
Sep 1988 |
|
EP |
|
2277826 |
|
Feb 1976 |
|
FR |
|
2513750 |
|
Oct 1975 |
|
DE |
|
2122188 |
|
Jan 1984 |
|
GB |
|
Primary Examiner: Ford; John M.
Attorney, Agent or Firm: Oblon, Spivak, McClelland, Maier,
& Neustadt
Claims
We claim:
1. A pyrazole derivative of the formula I
wherein
A is a C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.4 alkenyl
group or a C.sub.2 -C.sub.4 alkynyl group;
B is a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group, a halogen
atom, a C.sub.1 -C.sub.3 haloalkyl group, a C.sub.1 -C.sub.3 alkoxy
group, a C.sub.1 -C.sub.3 alkylthio group, a C.sub.2 -C.sub.4
alkoxyalkyl group, a C.sub.2 -C.sub.4 alkylthioalkyl group or a
C.sub.2 -C.sub.4 alkoxycarbonyl group;
X is a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy
group, a halogen atom, a nitro group, a cyano group, a C.sub.1
-C.sub.6 haloalkyl group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a
C.sub.2 -C.sub.6 alkylcarbonyl group, a C.sub.2 -C.sub.6
alkoxycarbonyl group, an aminocarbonyl group substituted
independently by hydrogen or by a C.sub.1 -C.sub.6 alkyl group, a
C.sub.1 -C.sub.6 haloalkoxy group, a C.sub.1 -C.sub.6 alkylthio
group or a C.sub.2 -C.sub.6 alkylthioalkyl group;
Y is --OR.sup.1 (wherein R.sup.1 is a C.sub.3 -C.sub.8 cycloalkyl
group, a C.sub.4 -C.sub.8 cycloalkylalkyl group, a C.sub.3 -C.sub.6
alkenyl group, a C.sub.2 -C.sub.6 alkynyl group, a C.sub.1 -C.sub.6
haloalkyl group, a C.sub.3 -C.sub.8 halocycloalkylalkyl group, a
C.sub.3 -C.sub.6 haloalkenyl group, a C.sub.2 -C.sub.6 haloalkynyl
group, .Iadd.or a C.sub.2 -C.sub.6 nitroalkyl group) .Iaddend..[.a
C.sub.2 -C.sub.6 nitroalkyl group or a phenyl group which may be
substituted by a C.sub.1 -C.sub.3 alkyl group, a halogen atom, a
nitro group or a C.sub.1 -C.sub.3 alkoxy group).].,
--O--L--O--R.sup.1 (wherein L is a C.sub.1 -C.sub.6 alkylene group
which may be substituted by a C.sub.1 -C.sub.3 alkyl group, and
R.sup.1 is as defined above), --O--L--OH (wherein L is as defined
above), --O--L--O--L--O--R.sup.2 (wherein L is as defined above,
and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a
phenyl group which may be substituted by a C.sub.1 -C.sub.3 alkyl
group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy
group), --O--L--R.sup.3 (wherein L is as defined above, and R.sup.3
is a phenyl group which may be substituted by a C.sub.1 -C.sub.3
alkyl group, a halogen atom, a nitro group Or a C.sub.1 -C.sub.3
alkoxy group), --O--M (wherein M is a 3- to 6-membered alicyclic
group containing not more than two sulfur or oxygen atoms and
formed by a linkage of from 1 to 4 carbon atoms), --O--L--M
(wherein L and M are as defined above), --O--L--NR.sup.4 R.sup.5
(wherein L is as defined above and each of R.sup.4 and R.sup.5
which may be the same or different is a hydrogen atom or a C.sub.1
-C.sub.6 alkyl group, or R.sup.4 and R.sup.5 form a 6-membered ring
together with the adjacent nitrogen atom), --O--L--COOR.sup.4
(wherein L and R.sup.4 are as defined above),
--O--CH.dbd.CH--COOR.sup.4 (wherein R.sup.4 is as defined above),
--O--L--CN (wherein L is as defined above), --O--L--C(O)--R.sup.2
(wherein L and R.sup.2 are as defined above), --O--L--S(O).sub.n
--R.sup.4 (wherein L and R.sup.4 are as defined above, and n is an
integer of from 0 to 2), --O--COOR.sup.4 (wherein R.sup.4 are as
defined above), --O--CONR.sup.4 R.sup.5 (wherein R.sup. 4 and
R.sup.5 are as defined above), .Iadd.or
.Iaddend.--OP(O)(OR.sup.4).sub.2 (wherein R.sup.4 is as defined
above), .[.--S(O).sub.n R.sup.1 (wherein R.sup.1 and n are as
defined above), or --S(O).sub.n --L--O--R.sup.1 (wherein L, R.sup.1
and n are as defined above).].;
Z is a halogen atom, a nitro group, a C.sub.1 -C.sub.3 alkoxy
group, a trifluoromethyl group, a trifluoromethoxy group, a cyano
group or --S(O).sub.n R.sup.6 (wherein n is as defined above, and
R.sup.6 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3
haloalkyl group);
V is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group or a C.sub.1 -C.sub.4 alkoxy group;
W is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.4
alkoxy group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a C.sub.2
-C.sub.5 alkoxycarbonyl group, a C.sub.1 -C.sub.3 haloalkoxy group,
a nitro group, a cyano group or --S(O).sub.n --R.sup.6 (wherein n
and R.sup.6 are as defined above) and
Q is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group which may be
substituted by a halogen atom, a C.sub.1 -C.sub.6 alkenyl group
which may be substituted by a halogen atom, a C.sub.1 -C.sub.6
alkynyl group which may be substituted by a halogen atom, a
cyanomethyl group, --C(O)--R.sup.7 (wherein R.sup.7 is a phenyl
group which may be substituted by the same or different
substituents selected from the group consisting of a C.sub.1
-C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkenyl group, a C.sub.1
-C.sub.6 alkynyl group, a C.sub.1 -C.sub.6 haloalkyl group, a
C.sub.1 -C.sub.6 haloalkenyl group, a C.sub.1 -C.sub.6 haloalkynyl
group, a halogen atom, a nitro group and a trifluoromethyl group, a
C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, or a
hydroxyl group), --S(O).sub.2 R.sup.7 (wherein R.sup.7 is as
defined above), --P(O)(OR.sup.7).sub.2 (wherein R.sup.7 is as
defined above), --L--C(O)--R.sup.7 (wherein L and R.sup.7 are as
defined above), --L--C(O)--N(R.sup.8)(R.sup.9) (wherein L is as
defined above, and each of R.sup.8 and R.sup.9 which may be the
same or different is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl
group), --L--R.sup.10 (wherein L is as defined above, and R.sup.10
is a phenyl group which may be substituted by the same or different
substituents selected from the group consisting of a halogen atom,
a nitro group and a trifluoromethyl group, a C.sub.1 -C.sub.6 alkyl
group, a C.sub.1 -C.sub.6 alkoxy group, or a hydroxyl group),
--L--N(R.sup.8)(R.sup.9) (wherein L, R.sup.8 and R.sup.9 are as
defined above), --L--OR.sup.11 (wherein L is as defined above, and
R.sup.11 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, or a
C.sub.1 -C.sub.6 alkenyl group), --L--OC(O)R.sup.12 (wherein L is
as defined above, and R.sup.12 is a C.sub.1 -C.sub.6 alkyl group or
a C.sub.1 -C.sub.6 alkoxy group), --L--S(O).sub.n R.sup.11 (wherein
L, n and R.sup.11 are as defined above), --L--SC(O)R.sup.8 (wherein
L and R.sup.8 are as defined above), ##STR42## (wherein each of L1
and L2 which may be the same or different is a methylene group, an
oxygen atom or a sulfur atom, R.sup.12 is a hydrogen atom or a
C.sub.1 -C.sub.3 alkyl group, and m is 2 or 3); and a salt
thereof.
2. .[.The.]. .Iadd.A .Iaddend.pyrazole derivative of the formula I
.[.according to claim 1.]., ##STR43## wherein A, B, X, Y, Z and Q
are as follows:
A: Me, Et, n-Pr, i-Pr, CH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 C.tbd.CH,
t-Bu
B: H, Me, Et, n-Pr, i-Pr, Cl, Br, CH.sub.2 Cl, CF.sub.3, OMe, OEt,
OPr-i, SMe, CH.sub.2 OMe, CH.sub.2 SMe, CO.sub.2 Me, CO.sub.2
Et
X: Me, Et, n-Pr, i-Pr, n-Bu, i-Bu, S-Bu, t-Bu, OMe, OEt, OPr-n,
OPr-i, OBu-n, OBu-i, OBu-s, OBu-t, F, Cl, Br, I, NO.sub.2, CN,
CH.sub.2 F, CHF.sub.2, CF.sub.3, CH.sub.2 CF.sub.3, CHCl,
CCl.sub.3, CHClMe, CH.sub.2 CH.sub.2 Cl, CHClCH.sub.2 Cl, CH.sub.2
Br, CHBrMe, CH.sub.2 CH.sub.2 Br, CH.sub.2 CH.sub.2 Br, CH.sub.2
OMe, CH.sub.2 OEt, CH.sub.2 OPr-n, CH.sub.2 OPr-i, CH.sub.2 OBu-n,
CH.sub.2 OBu-i, CH.sub.2 OBu-s, CH.sub.2 OBu-t, CHMeOMe, CHMeOEt,
CHMeOPr-n, CHMeOPr-i, CHMeOBu-n, CHMeOBu-i, CHMeOBu-s, CHMeOBu-t,
CH.sub.2 CH.sub.2 OMe, CH.sub.2 CH.sub.2 OEt, CH.sub.2 CH.sub.2
OPr-i, Ac, COEt, COPr-n, COPr-i, COOMe, COOEt, COOPr-i, CONHMe,
CONHEt, CONMe.sub.2, CONEt.sub.2, CONEtMe, OCHF.sub.2, OCF.sub.3,
OCH.sub.2 CF.sub.3, SMe, SEt, CH.sub.2 SMe, CH.sub.2 SEt, CHMeSMe,
CHMeSEt
Y: ##STR44## OCHMeCH.dbd.CH.sub.2, OCMe.sub.2 CH.dbd.CH.sub.2,
OCH.sub.2 CMe.dbd.CH.sub.2, OCH.sub.2 CH.dbd.CHMe, OCH.sub.2
CH.dbd.CMe.sub.2, OCH.sub.2 C.tbd.CH, OCHMeC.tbd.CH, OCMe.sub.2
C.tbd.CH, OCH.sub.2 C.tbd.CMe, OCH.sub.2 CH.sub.2 F, OCH.sub.2
CHF.sub.2, OCH.sub.2 CF.sub.3, OCH.sub.2 CH.sub.2 Cl, OCHMeCH.sub.2
Cl, OCH.sub.2 CCl.sub.3, OCH.sub.2 CH.sub.2 CH.sub.2 Cl, OCH.sub.2
CH.sub.2 Br, ##STR45## OCH.sub.2 CCl.dbd.CH.sub.2, OCH.sub.2
CH.sub.2 CH.dbd.CH.sub.2, OCH.sub.2 CCl.dbd.CHCl, OCH.sub.2
CH.sub.2 NO.sub.2, .[.OPh, OPh-Me-2 OPh-Cl-4, OPh-NO.sub.2 -4, .].
OCH.sub.2 CH.sub.2 OMe, OCH.sub.2 CH.sub.2 OEt, OCH.sub.2 CH.sub.2
OPr-n, OCH.sub.2 CH.sub.2 OPr-i, OCH.sub.2 CH.sub.2 OBu-N,
OCH.sub.2 CH.sub.2 OBu-i, OCH.sub.2 CH.sub.2 Bu-s, OCH.sub.2
CH.sub.2 OBu-t, OCHMeCH.sub.2 OMe, OCH.sub.2 CH.sub.2 OPh,
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe, OCH.sub.2 CH.sub.2 OH,
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe, OCH.sub.2 Ph, OCHMePh,
OCH.sub.2 Ph-4-Me, OCH.sub.2 Ph-4-Cl, OCH.sub.2 CH.sub.2 Ph,
##STR46## OCH.sub.2 CH.sub.2 NH.sub.2, OCH.sub.2 CH.sub.2 NHMe,
OCH.sub.2 CH.sub.2 NMe.sub.2, OCH.sub.2 CH.sub.2 NEt.sub.2,
##STR47## OCH.sub.2 COOMe, OCH.sub.2 COOEt, OCH.sub.2 COOPr-n,
OCH.sub.2 COOPr-i, OCH.sub.2 COOBu-t, OCHMeCOOMe, OCHMeCOOEt
OCHMeCOOPr-n, OCHMeCOOPr-i, OCHMeCOOBu-t, OCH.sub.2 CH.sub.2 CN,
OCH.sub.2 CN, OCHMeCN, OCH.sub.2 SMe, OCH.sub.2 C(O)Ph, OCH.sub.2
C(O)Me, OCH.sub.2 CH.sub.2 SMe, OCH.sub.2 CH.sub.2 SOMe, OCH.sub.2
CH.sub.2 SO.sub.2 Me, OCH.sub.2 CH.sub.2 SEt, OCH.sub.2 CH.sub.2
SO.sub.2 Et, OCOOMe, OCOOEt, OCOOPr-i, OCONH.sub.2, OCONHMe,
OCONMe.sub.2, OP(O)(OMe).sub.2, OP(O)(OEt).sub.2, ##STR48##
.[.SCH.sub.2 CH.dbd.CH.sub.2, SCH.sub.2 C.tbd.CH, SCH.sub.2
CF.sub.3, SCH.sub.2 CH.sub.2 Cl, SCH.sub.2 CCl.sub.3,.]. ##STR49##
.[.SPh,SCH.sub.2 CH.sub.2 OMe, SCH.sub.2 CH.sub.2 OEt, SCH.sub.2
CH.sub.2 OPr-i, SCH.sub.2 CH.sub.2 OPh,.]. ##STR50##
.[.S(O)CH.sub.2 CH.dbd.CH.sub.2, .].2CH.tbd.CH, S(O)CH.sub.2
CF.sub.3, S(O)CH.sub.2 CH.sub.2 Cl, S(O)CH.sub.2 ##STR51##
.[.S(O)Ph, S(O)CH.sub.2 CH.sub.2 OMe, S(O)CH.sub.2 CH.sub.2 OEt,
S(O)CH.sub.2 CH.sub.2 OPr-i, S(O)CH.sub.2 CH.sub.2 OPh,.].
##STR52## .[.SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2, SO.sub.2 CH.sub.2
C.tbd.CH, SO.sub.2 CH.sub.2 CF.sub.3, SO.sub.2 CH.sub.2 CH.sub.2
Cl, SO.sub.2 CH.sub.2 .]. ##STR53## .[.SO.sub.2 Ph, SO.sub.2
CH.sub.2 CH.sub.2 OMe, SO.sub.2 CH.sub.2 CH.sub.2 OEt, SO.sub.2
CH.sub.2 CH.sub.2 OPr-i, .].
Z: F, Cl, Br, I, NO.sub.2, OMe, OEt, OPr-n, OPr-I, CF.sub.3, CN,
SMe, SOMe, SO.sub.2 Me, SCF.sub.3, SOCF.sub.3, SO.sub.2
CF.sub.3
Q H, Me, Et, n-Pr, i-Pr, n-Bu, i-Bu, s-Bu, t-Bu, CH.sub.2 CH.sub.2
Cl, CH.sub.2 CF.sub.3, CHClMe, CH.sub.2 CH.sub.2 Br, CHClCH.sub.2
Cl, CH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 CMe.dbd.CH.sub.2, CH.sub.2
CH=CHMe, CH.sub.2 C.tbd.CH, CH.sub.2 CCl.dbd.CH.sub.2, CH.sub.2 CN,
CH.sub.2 Ph, CH.sub.2 Ph-Cl-2, CH.sub.2 Ph-Cl-3, CH.sub.2 Ph-Me-2,
##STR54## CH.sub.2 Ph-Me.sub.2 -2,4, CH.sub.2 Ph-Me-4, CHMePh,
CHEtPh, CH.sub.2 Ph-NO.sub.2 -2, CH.sub.2 Ph-CF.sub.3 -3, CH.sub.2
OMe, CH.sub.2 OEt, CH.sub.2 OH, CHMeOH, CH.sub.2 NHMe, CH.sub.2
NMe.sub.2, CHMeNMe.sub.2, CH.sub.2 COPh, CH.sub.2 COPh-NO.sub.2 -4,
CH.sub.2 COPh-Me-4, CH.sub.2 COPh-Cl-4, CH.sub.2 COPh-Me-2,4,
CH.sub.2 COPh-CF.sub.3 -4, CH.sub.2 Ac, CH.sub.2 COEt, CHMeAc,
CH.sub.2 CO.sub.2 Me, CH.sub.2 CO.sub.2 Et, CH.sub.2 CO.sub.2 Pr-n,
CH.sub.2 COPr-i, CH.sub.2 CO.sub.2 Bu-t, CH.sub.2 CO.sub.2 H,
CHMeCO.sub.2 H, CH.sub.2 CONHMe, CH.sub.2 CONMe.sub.2, CH.sub.2
CONHEt, CH.sub.2 CONEt.sub.2, CH.sub.2 CONPr-n.sub.2, CH.sub.2
OCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 OAc, CH.sub.2 COEt, CH.sub.2
COPr-i, CH.sub.2 COBu-t, CH.sub.2 OCO.sub.2 Me, CH.sub.2 OCO.sub.2
Et, CH.sub.2 OCO.sub.2 Pr-i, CH.sub.2 OCO.sub.2 Bu-t, CH.sub.2 SMe,
CH.sub.2 SEt, CH.sub.2 SCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 SAc,
CH.sub.2 SCOBu-t, CH.sub.2 SO.sub.2 Me, CH.sub.2 SO.sub.2 Et,
CH.sub.2 SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2, COPh, COPh-Me-4,
COPh-NO.sub.2 -2, COPh-Cl.sub.2 -2,4, Ac, COEt, COPr-n, COPr-i,
COBu-n, COBu-t, CO.sub.2 Me, CO.sub.2 Et, CO.sub.2 Bu-t, CO.sub.2
Pr-i, CO.sub.2 Ph, SO.sub.2 Me, SO.sub.2 Et, SO.sub.2 Ph, SO.sub.2
Ph-Me-4, SO.sub.2 Ph-Cl-4, SO.sub.2 Ph-(NO.sub.2).sub.2 -2,4,
P(.dbd.O)(OMe).sub.2, P(.dbd.O)(OEt).sub.2, P(.dbd.O)(OPr-n).sub.2,
P(.dbd.O)(OPr-i).sub.2, P(.dbd.O)OMeOPh;
and a salt thereof.
3. A selective herbicidal composition comprising a herbicidally
effective amount of a pyrazole derivative of the formula I as
defined in claim 1 or its salt and an agricultural carrier or
diluent.
4. A method for controlling weeds, which comprise applying a
herbicidally effective amount of a pyrazole derivative of the
formula I as defined in claim 1 or its salt to a locus to be
protected.
5. A pyrazole derivative of the formula I ##STR55## wherein A is a
C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.4 alkenyl group or a
C.sub.2 -C.sub.4 alkynyl group;
B is a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group, a halogen
atom, a C.sub.1 -C.sub.3 haloalkyl group, a C.sub.1 -C.sub.3 alkoxy
group, a C.sub.1 -C.sub.3 alkylthio group, a C.sub.2 -C.sub.4
alkoxyalkyl group, a C.sub.2 -C.sub.4 alkylthioalkyl group or a
C.sub.2 -C.sub.4 alkoxycarbonyl group;
X is a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy
group, a halogen atom, a nitro group, a cyano group, a C.sub.1
-C.sub.6 haloalkyl group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a
C.sub.2 -C.sub.6 alkylcarbonyl group, a C.sub.2 -C.sub.6
alkoxycarbonyl group, an aminocarbonyl group substituted
independently by hydrogen or by a C.sub.1 -C.sub.6 alkyl group, a
C.sub.1 -C.sub.6 haloalkoxy group, a C.sub.1 -C.sub.6 alkylthio
group or a C.sub.2 -C.sub.6 alkylthioalkyl group;
Y is --OR.sup.1 (wherein R.sup.1 is a C.sub.3 -C.sub.8 cycloalkyl
group, a C.sub.4 -C.sub.8 cycloalkylalkyl group, a C.sub.3 -C.sub.6
alkenyl group, a C.sub.2 -C.sub.6 alkynyl group, a C.sub.1 -C.sub.6
haloalkyl group, a C.sub.3 -C.sub.8 halocycloalkylalkyl group, a
C.sub.3 -C.sub.6 haloalkenyl group, a C.sub.2 -C.sub.6 haloalkynyl
group, a C.sub.2 -C.sub.6 nitroalkyl group or a phenyl group which
may be substituted by a C.sub.1 -C.sub.3 alkyl group, a halogen
atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy group),
--O--L--O--R.sup.1 (wherein L is a C.sub.1 -C.sub.6 alkylene group
which may be substituted by a C.sub.1 -C.sub.3 alkyl group, and
R.sup.1 is as defined above), --O--L--OH (wherein L is as defined
above), --O--L--O--L--O--R.sup.2 (wherein L is as defined above,
and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a
phenyl group which may be substituted by a C.sub.1 -C.sub.3 alkyl
group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy
group), --O--L--R.sup.3 (wherein L is as defined above, and R.sup.3
is a phenyl group which may be substituted by a C.sub.1 -C.sub.3
alkyl group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3
alkoxy group), --O--M (wherein M is a 3- to 6-membered alicyclic
group containing not more than two sulfur or oxygen atoms and
formed by a linkage of from 1 to 4 carbon atoms), --O--L--M
(wherein L and M are as defined above), --O--L--NR.sup.4 R.sup.5
(wherein L is as defined above and each of R.sup.4 and R.sup.5
which may be the same or different is a hydrogen atom or a C.sub.1
-C.sub.6 alkyl group, or R.sup.4 and R.sup.5 form a 6-membered ring
together with the adjacent nitrogen atom), --O--L--COOR.sup.4
(wherein L and R.sup.4 are as defined above),
--O--CH.dbd.CH--COOR.sup.4 (wherein R.sup.4 is as defined above),
--O--L--CN (wherein L is as defined above), --O--L--C(O)--R.sup.2
(wherein L and R.sup.2 are as defined above), --O--L--S(O).sub.n
--R.sup.4 (wherein L and R.sup.4 are as defined above, and n is an
integer of from 0 to 2), --O--COOR.sup.4 (wherein R.sup.4 is as
defined above), --O--CONR.sup.4 R.sup.5 (wherein R.sup.4 and
R.sup.5 are as defined above), --OP(O)(OR.sup.4).sub.2 (wherein
R.sup.4 is as defined above), --S(O).sub.n R.sup.1 (wherein R.sup.1
and n are as defined above), or --S(O).sub.n --L--O--R.sup.1
(wherein L, R.sup.1 and n are as defined above);
Z is a halogen atom, a nitro group, a C.sub.1 -C.sub.3 alkoxy
group, a trifluoromethyl group, a trifluoromethoxy group, a cyano
group or --S(O).sub.n R.sup.6 (wherein n is as defined above, and
R.sup.6 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3
haloalkyl group);
V is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group or a C.sub.1 -C.sub.4 alkoxy group;
W is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.4
alkoxy group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a C.sub.2
-C.sub.5 alkoxycarbonyl group, a C.sub.1 -C.sub.3 haloalkoxy group,
a nitro group, a cyano group or --S(O).sub.n --R.sup.6 (wherein n
and R.sup.6 are as defined above); and
Q is selected from the group consisting of CH.sub.2 NHCH.sub.2
CH.dbd.CH.sub.2, CH.sub.2 NMeCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2
NHAc, CH.sub.2 NHCOEt, CH.sub.2 NHCO.sub.2 Me, CH.sub.2 NHCO.sub.2
Et, CH.sub.2 NMeCO.sub.2 Me, COCH.sub.2 Cl, COCHCl.sub.2,
COCCl.sub.3, COCF.sub.3, COCH.sub.2 OMe, COCH.sub.2 OPh, COCH.sub.2
CH.dbd.CHCH.sub.3, CONHMe, CONMe.sub.2, CONHEt, CONEt.sub.2,
CONPr-n.sub.2, CON(CH.sub.2 CH.dbd.CH.sub.2).sub.2, CONMePh,
##STR56## CO.sub.2 CH.sub.2 Ph, SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2,
SO.sub.2 CF.sub.3, P(.dbd.S)(OMe).sub.2, P(.dbd.S)(OEt).sub.2,
P(.dbd.O)(OCH.sub.2 CH.dbd.CH.sub.2).sub.2, P(.dbd.O)OPhOCH.sub.2
CH.dbd.CH.sub.2 ; and salts thereof. .Iadd.
6. A pyrazole derivative of the formula I ##STR57## .Iaddend.
wherein
A is a C.sub.1 -C.sub.4 -group, a C.sub.2 -C.sub.4 -alkenyl group,
or a C.sub.2 -C.sub.4 alkynyl group;
B is a hydrogen, a C.sub.1 -C.sub.3 alkyl group, a halogen atom, a
C.sub.1 -C.sub.3 -haloalkyl group, a C.sub.1 -C.sub.3 -alkoxy
group, a C.sub.1 -C.sub.3 -alkylthio group, a C.sub.2 -C.sub.4
-alkoxyalkyl group, a C.sub.2 -C.sub.4 -alkylthioalkyl group or
C.sub.2 -C.sub.4 -alkoxycarbonyl group;
X is a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.6 -alkoxy
group, a halogen atom, a nitro group, a cyano group, a C.sub.1
-C.sub.6 -haloalkyl group, a C.sub.2 -C.sub.6 -alkoxyalkyl group, a
C.sub.2 -C.sub.6 -alkylcarbonyl group, a C.sub.2 -C.sub.6
-alkoxycarbonyl group, an aminocarbonyl group substituted
independently by hydrogen or by a C.sub.1 -C.sub.6 -alkyl group, a
C.sub.1 -C.sub.6 -haloalkoxy group, a C.sub.1 -C.sub.6 -alkylthio
group or a C.sub.2 -C.sub.6 -alkylthioalkyl group;
Y is --OR.sup.1 (wherein R.sup.1 is a C.sub.3 -C.sub.8 -cycloalkyl
group, a C.sub.4 -C.sub.8 -cycloalkylalkyl group, a C.sub.3
-C.sub.6 -alkenyl group, a C.sub.2 -C.sub.6 -alkynyl group, a
C.sub.1 -C.sub.6 haloalkyl group, a C.sub.3 -C.sub.8
-halocycloalkylalkyl group, a C.sub.3 -C.sub.6 haloalkenyl group, a
C.sub.2 -C.sub.6 haloalkynyl group, or a C.sub.2 -C.sub.6
nitroalkyl group), --O--L--O--R (wherein L is a C.sub.1 -C.sub.6
alkylene gorup which may be substituted by a C.sub.1 -C.sub.3 alkyl
group, and R is a C.sub.1 -C.sub.4 alkyl group), --O--L--O--R.sup.1
(wherein L is a C.sub.1 -C.sub.6 alkylene group which may be
substituted by a C.sub.1 -C.sub.3 -alkyl group, and R.sup.1 is as
defined above), --O--L--OH (wherein L is as defined above),
O--L--O--L--O--R.sup.2 (wherein L is as defined above, and R.sup.2
is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a phenyl
group which may be substituted by a C.sub.1 -C.sub.3 alkyl group, a
halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy group),
--O--L--R.sup.3 (wherein L is as deined above, and R.sup.3 is a
phenyl group which may be substituted by a C.sub.1 -C.sub.3 alkyl
group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy
group), --O--M (wherein M is a 3- to 6-membered alicyclic group
containing not more than two sulfur or oxygen atoms and formed by a
linkage of from 1 to 4 carbon atoms), O--L--M (wherein L and M are
as defined above), --O--L--NR.sup.4 R.sup.5 (wherein L is as
defined above and each of R.sup.4 and R.sup.5 which may be the same
or different is a hydrogen atom or a C.sub.1 -C.sub. 6 alkyl group,
or R.sup.4 and R.sup.5 form a 6-membered ring together with the
adjacent nitrogen atom), --O--L--COOR.sup.4 (wherein L and R.sup.4
are as defined above), --O--CH.dbd.CH--COOR.sup.4 (wherein R.sup.4
is as defined above), --O--L--CN (wherein L is as defined
above)--O--L--C(O)--R.sup.2 (wherein L and R.sup.2 are as defined
above), --O--L--S(O).sub.n --R.sup.4 (wherein L and R.sup.4 are as
defined above, and n is an integer of from 0 to 2) --O--COOR.sup.4
(wherein R.sup.4 are as defined above), --O--CONR.sup.4 R.sup.5
(wherein R.sup.4 and R.sup.5 are as defined above, or
--OP(O)(OR.sup.4).sub.2 (wherein R.sup.4 is as defined above);
Z is a halogen atom, a nitro group, a C.sub.1 -C.sub.3 alkoxy
group, a trifluoromethylgroup, a trifluoromethoxy group, a cyano
group or --S(O).sub.n R.sup.6 (wherein n is as defined above, and
R.sup.6 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3
haloalkyl group);
V is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group or a C.sub.1 -C.sub.4 alkoxy group;
W is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.4
alkoxy group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a C.sub.2
-C.sub.5 alkoxycarbonyl group, a C.sub.1 -C.sub.3 haloalkoxy group,
a nitro group, a cyano group or --S(O).sub.n --R.sup.6 (wherein n
and R.sup.6 are as defined above) and
O is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group which may be
substituted by a halogen atom, a C.sub.1 -C.sub.6 alkenyl group
which may be substituted by a halogen atom, a C.sub.1 -C.sub.6
alkynyl group which may be substituted by a halogen atom, a
cyanomethyl group --C(O)--R.sup.7 (wherein R.sup.7 is a phenyl
group which may be substituted by the same or different
substituents selected from the group consisting of a C.sub.1
-C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkenyl group, a C.sub.1
-C.sub.6 alkynyl group, a C.sub.1 -C.sub.6 haloalkyl group, a
C.sub.1 -C.sub.6 haloalkenyl group, a C.sub.1 -C.sub.6 haloalkynyl
group, a halogen atom, a nitro group and a trifluoromethyl group, a
C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, or a
hydroxyl group), --S(O).sub.2 R.sup.7 (wherein R.sup.7 is as
defined above), --P(O)(OR.sup.7).sub.2 (wherein R.sup.7 is as
defined above, --L--C(O)--R.sup.7 (wherein L and R.sup.7 are as
defined above, --L--C--(O)--N(R.sup.8)(R.sup.9)(wherein L is as
defined above, and each of R.sup.8 and R.sup.9 which may be the
same or different is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl
group), --L--R.sup.10 (wherein L is as defined above, and R.sup.10
is a phenyl group which may be substituted by the same or different
substituents selected from the group consisting of a halogen atom,
a nitro group and a trifluoromethyl group, a C.sub.1 -C.sub.6 alkyl
group, a C.sub.1 -C.sub.6 alkoxy group, or a hydroxy group),
--L--N(R.sup.8)(R.sup.9) (wherein L, R.sup.8 and R.sup.9 are as
defined above), --L--OR.sup.11 (wherein L is as defined above, and
R.sup.11 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, or a
C.sub.1 -C.sub.6 alkenyl group), --L--OC(O)R.sup.12 (wherein L is
as defined above, and R.sup.12 is a C.sub.1 -C.sub.6 alkyl group or
a C.sub.1 -C.sub.6 alkoxy group), --L--S(O).sub.n R.sup.11 (wherein
L, n and R.sup.11 are as defined above, --L--SC(O)R.sup.8 (wherein
L and R.sup.8 are as defined above), ##STR58## (wherein each of L1
and L2 which may be the same or different is a methylene group, an
oxygen atom or a sulfur atom, R.sup.12 is a hydrogen atom or a
C.sub.1 -C.sub.3 alkyl gropu, and m is 2 or 3); and a salt thereof.
.Iadd.
7. A pyrazole derivative of the formula I ##STR59## .Iaddend. A is
a C.sub.1 -C.sub.4 - alkyl group, a C.sub.2 -C.sub.4 -alkenyl
group, or a C.sub.2 -C.sub.4 alkynyl group;
B is a hydrogen, a C.sub.1 -C.sub.3 alkyl group, a halogen atom, a
C.sub.1 -C.sub.3 -haloalkyl group, a C.sub.1 -C.sub.3 -alkoxy
group, a C.sub.1 -C.sub.3 -alkylthio group, a C.sub.2 -C.sub.4
-alkoxyalkyl group, a C.sub.2 -C.sub.4 -alkylthioalkyl group or
C.sub.2 -C.sub.4 -alkoxycarbonyl group;
X is a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.6 -alkoxy
group, a halogen atom, a nitro group, a cyano group, a C.sub.1
-C.sub.6 -haloalkyl group, a C.sub.2 -C.sub.6 -alkoxyalkyl group, a
C.sub.2 -C.sub.6 -alkylcarbonyl group, a C.sub.2 -C.sub.6
-alkoxycarbonyl group, an aminocarbonyl group substituted
independently by hydrogen or by a C.sub.1 -C.sub.6 -alkyl group, a
C.sub.1 -C.sub.6 -haloalkoxy group, a C.sub.1 -C.sub.6 -alkylthio
group or a C.sub.2 -C.sub.6 -alkylthioalkyl group;
Y is --OR.sup.1 (wherein R.sup.1 is a C.sub.3 -C.sub.8 -cycloalkyl
group, C.sub.4 -C.sub.8 -cycloalkylalkyl group, a C.sub.3 -C.sub.6
-alkenyl group, a C.sub.2 -C.sub.6 -alkynyl group, a C.sub.3
-C.sub.8 -halocycloalkylalkyl group, a C.sub.3 -C.sub.6 haloalkenyl
group, a C.sub.2 -C.sub.6 haloalkynyl group, or a C.sub.2 -C.sub.6
nitroalkyl group), --O--L--O--R (wherein L is a C.sub.1 -C.sub.6
alkylene group which may be substituted by a C.sub.1 -C.sub.3 alkyl
group, and R is a C.sub.1 -C.sub.4 alkyl group), --O--L--O--R.sup.1
(wherein L is a C.sub.1 -C.sub.6 alkylene group which may be
substituted by a C.sub.1 -C.sub.3 -alkyl group, and R.sup.1 is as
defined above), --O--L--OH (wherein L is as defined above),
O--L--O--L--O--R.sup.2 (wherein L is as defined above, and R.sup.2
is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a phenyl
group which may be substituted by a C.sub.1 -C.sub.3 alkyl group, a
halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy group),
--O--L--R.sup.3 (wherein L is as defined above, and R.sup.3 is a
phenyl group which may be substituted by a C.sub.1 -C.sub.3 alkyl
group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy
group), --O--M (wherein M is a 3- to 6-membered alicyclic group
containing not more than two sulfur or oxygen atoms and formed by a
linkage of from 1 to 4 carbon atoms), O--L--M (wherein L and M are
as defined above), O--L--NR.sup.4 R.sup.5 (wherein L is as defined
above and each of R.sup.4 and R.sup.5 which may be the same or
different is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, or
R.sup.4 and R.sup.5 form a 6-membered ring together with the
adjacent nitrogen atom), --O--L--COOR.sup.4 (wherein L and R.sup.4
are as defined above), --O--CH.dbd.CH--COOR.sup.4 (wherein R.sup.4
is as defined above), --O--L--CN (wherein L is as defined above),
--O--L--C(O)-R.sup.2 (wherein L and R.sup.2 are as defined above,
and n is an integer of from 0 to 2), --O--COOR.sup.4 (wherein
R.sup.4 are as defined above), --O--CONR.sup.4 R.sup.5 (wherein
R.sup.4 and R.sup.5 are as defined above, or
--OP(O)(OR.sup.4).sub.2 (wherein R.sup.4 is as defined above);
Z is a halogen atom, a nitro group, a C.sub.1 -C.sub.3 alkoxy
group, a trifluoromethyl group, a trifluoromethoxy group, a cyano
group or --S(O).sub.n R.sup.6 (wherein n is as defined above, and
R.sup.6 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3
haloalkyl group);
V is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group or a C.sub.1 -C.sub.4 alkoxy group;
W is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.4
alkoxy group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a C.sub.2
-C.sub.5 alkoxycarbonyl group, a C.sub.1 -C.sub.3 haloalkoxy group,
a nitro group, a cyano group or --S(O).sub.n --R.sup.6 (wherein n
and R.sup.6 are as defined above) and
O is selected from the group consisting of CH.sub.2 NHCH.sub.2
CH.dbd.CH.sub.2, CH.sub.2 NMeCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2
NHAc, CH.sub.2 NHCOEt, CH.sub.2 NHCO.sub.2 Me, CH.sub.2 NHCO.sub.2
Et, CH.sub.2 NMeCO.sub.2 Me, COCH.sub.2 Cl, COCHCl.sub.2,
COCCl.sub.3, COCF.sub.3, COCH.sub.2 OMe, COCH.sub.2 OPh, COCH.sub.2
CH.dbd.CHCH.sub.3, CONHMe, CONMe.sub.2, CONHEt, CONEt.sub.2,
CONPr-n.sub.2, CON(CH.sub.2 CH.dbd.CH.sub.2).sub.2, CONMePh,
##STR60## CO.sub.2 CH.sub.2 Ph, SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2,
SO.sub.2 CF.sub.3, P(.dbd.S) (OMe).sub.2, P(.dbd.S) (OEt).sub.2,
P(.dbd.O)-(OCH.sub.2 CH.dbd.CH.sub.2).sub.2, P(.dbd.O)OPHOCH.sub.2
CH.dbd.CH.sub.2 ; and salts thereof. .Iadd.
8. The pyrazole derivative of the formula I according to claim 6,
wherein A is ethyl, B is hydrogen, Q is hydrogen, X is Cl, Z is
SO.sub.2 Me, and Y is --O--L--O--R wherein L is a C.sub.2 alkylene
group which may be substituted by a methyl group and R is a
C.sub.1-4 alkyl group. .Iaddend. .Iadd.9. The pyrazole derivative
of the formula I according to claim 8, wherein Y is --OCH.sub.2
CH.sub.2 OMe, --OCH.sub.2 CH.sub.2 OEt, --OCH.sub.2 CH.sub.2 OPr-n,
--CH.sub.2 CH.sub.2 OPr-i, --OCH.sub.2 CH.sub.2 OBu-n, --OCH.sub.2
CH.sub.2 OBu-i, --OCH.sub.2 CH.sub.2 OBu-s, --OCH.sub.2 CH.sub.2
OBu-t, --OCMeCH.sub.2 OMe or --OCH.sub.2 CHMeOMe.
.Iaddend. 10. The pyrazole derivative of the formula I according to
claim 9, wherein Y is --OCH.sub.2 CH.sub.2 OMe.
Description
The present invention relates to novel 4-benzoylpyrazole
derivatives and selective herbicides containing such derivatives as
active ingredients, which are useful particularly as upland field
herbicides.
Various herbicides have been developed for practical use from
extensive research and development of herbicides for many years,
and such herbicides have contributed to a reduction of the labor
force required for controlling weeds or to improvement of the
productivity of agricultural or horticultural plants.
Even now, it is still desired to develop a new herbicide having
superior herbicidal properties. In particular, it is desired to
develp an agricultural or horticultural herbicide which is capable
of selectively controlling weeds without adversely affecting the
crop plant and at a low dose. However, conventional herbicides do
not necessarily provide such desired herbicidal properties.
On the other hand, certain compounds of 4-benzoylpyrazole
derivatives are known to have herbicidal activities. For example,
pyrazolate (common name) and pyrazoxyfen (common name) are
practically used as herbicides for paddy fields. While exhibiting
excellent herbicidal activities as paddy field herbicides, these
compounds are not suitable as upland herbicides since their
herbicidal activities are weak against weeds of upland fields.
Among 4-benzoylpyrazole derivatives, it is desired to develop a
superior compound useful as an upland field herbicide.
The present invention provides a pyrazole derivative having the
formula: ##STR3## wherein
A is a C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.4 alkenyl
group or a C.sub.2 -C.sub.4 alkynyl group;
B is a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group, a halogen
atom, a C.sub.1 -C.sub.3 haloalkyl group, a C.sub.1 -C.sub.3 alkoxy
group, a C.sub.1 -C.sub.3 alkylthio group, a C.sub.2 -C.sub.4
alkoxyalkyl group, a C.sub.2 -C.sub.4 alkylthioaalkyl group or a
C.sub.2 -C.sub.4 alkoxycarbonyl group;
X is a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy
group, a halogen atom, a nitro group, a cyano group, a C.sub.1
-C.sub.6 haloalkyl group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a
C.sub.2 -C.sub.6 alkylcarbonyl group, a C.sub.2 -C.sub.6
alkoxycarbonyl group, an aminocarbonyl group substituted
independently by hydrogen or by a C.sub.1 -C.sub.6 alkyl group, a
C.sub.1 -C.sub.6 haloalkoxy group, a C.sub.1 -C.sub.6 alkylthio
group or a C.sub.2 -C.sub.6 alkylthioalkyl group;
Y is --OR.sup.1 (Wherein R.sup.1 is a C.sub.3 -C.sub.8 cycloalkyl
group, a C.sub.4 -C.sub.8 cycloalkylalkyl group, a C.sub.3 -C.sub.6
alkenyl group, a C.sub.2 -C.sub.6 alkynyl group, a C.sub.1 -C.sub.6
haloalkyl group, a C.sub.3 C.sub.8 halocycloalkylalkyl group, a
C.sub.3 -C.sub.6 haloalkenyl group, a C.sub.2 -C.sub.6 haloalkynyl
group, a C.sub.2 -C.sub.6 nitroalkyl group or a phenyl group which
may be substituted by a C.sub.1-C.sub.3 alkyl group, a halogen
atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy group),
--O--L--O--R.sup.1 (Wherein L is a C.sub.1 -C.sub.6 alkylene group
which may be substituted by a C.sub.1 -C.sub.3 alkyl group, and
R.sub.1 is as defined above), --O--L--OH (wherein L is as defined
above), --O--L--O--L--O--R.sup.2 (wherein L is as defined above,
and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a
phenyl group which may be substituted by a C.sub.1 -C.sub.3 alkyl
group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3 alkoxy
group), --O--L--R.sup.3 (wherein L is as defined above, and R.sup.3
is a phenyl group which may be substituted by a C.sub.1 -C.sub.3
alkyl group, a halogen atom, a nitro group or a C.sub.1 -C.sub.3
alkoxy group), --O--M (wherein M is a 3- to 6-membered alicyclic
group containing not more than two sulfur or oxygen atoms and
formed by a linkage of from 1 to 4 carbon atoms), --O--L--M
(wherein L and M are as defined above), --O--L--NR.sup.4 R.sup.5
(wherein L is as defined above and each of R.sup.4 and R.sup.5
which may be the same or different is a hydrogen atom or a C.sub.1
-C.sub.6 alkyl group, or R.sup.4 and R.sup.5 form a ring together
with the adjacent nitrogen atom), --O--L-COOR.sup.4 (wherein L and
R.sup.4 are as defined above), --O--CH.dbd.CH--COOR.sup.4 (wherein
R.sup.4 is as defined above), --O--L--CN (wherein L is as defined
above), --O--L--C(O)--R.sup.2 (wherein L and R.sup.2 are as defined
above), --O--L--S(O).sub.n --R.sup.4 (wherein L and R.sup.4 are as
defined above, and n is an integer of from 0 to 2), --O--COOR.sup.4
(wherein R.sup.4 are as defined above), --O--CONR.sup.4 R.sup.5
(wherein R.sup.4 and R.sup.5 are as defined above),
--OP(O)(OR.sup.4).sub.2 (wherein R.sup.4 is as defined above),
--S(O).sub.n R.sup.1 (wherein R.sup.1 and n are as defined above),
or --S(O).sub.n --L--O--R.sup.1 (wherein L, R.sup.1 and n are as
defined above);
Z is a halogen atom, a nitro group, a C.sub.1 -C.sub.3 alkoxy
group, a trifluoromethyl group, a trifluoromethoxy group, a cyano
group or --S(O).sub.n R.sup.6 (wherein n is as defined above, and
R.sup.6 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3
haloalkyl group);
V is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group or a C.sub.1 -C.sub.4 alkoxy group;
W is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl
group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.4
alkoxy group, a C.sub.2 -C.sub.6 alkoxyalkyl group, a C.sub.2
-C.sub.5 alkoxycarbonyl group, a C.sub.1 -C.sub.3 haloalkoxy group,
a nitro group, a cyano group or --S(O).sub.n --R.sup.6 (wherein n
and R.sup.6 are as defined above); and
Q is a hydrogen atom, a C.sub.1 --C.sub.6 alkyl group which may be
substituted by a halogen atom, a C.sub.1 -C.sub.6 alkenyl group
which may be substituted by a halogen atom, a C.sub.1 -C.sub.6
alkynyl group which may be substituted by a halogen atom, a
cyanomethyl group, --C(O)--R.sup.7 (wherein R.sup.7 is a phenyl
group which may be substituted by the same or different
substituents selected from the group consisting of a C.sub.1
-C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkenyl group, a C.sub.1
-C.sub.6 alkynyl group, a C.sub.1 -C.sub.6 haloalkyl group, a
C.sub.1 -C.sub.6 haloalkenyl group, a C.sub.1 -C.sub.6 haloalkynyl
group, a halogen atom, a nitro group and a trifluoromethyl group, a
C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, or a
hydroxyl group), --S(O).sub.2 R.sup.7 (wherein R.sup.7 is as
defined above), --P(O)(OR.sup.7).sub.2 (wherein R.sup.7 is as
defined above), --L--C(O)--R.sup.7 (wherein L and R.sup.7 are as
defined above), --L--C(O)--N(R.sup.8)(R.sup.9) (wherein L is as
defined above, and each of R.sup.8 and R.sup.9 which may be the
same or different is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl
group), --L--R.sup.10 (wherein L is as defined above, and R.sup.10
is a phenyl group which may be substituted by the sam or different
substituents selected from the group consisting of a halogen atom,
a nitro group and a trifluoromethyl group, a C.sub.1 -C.sub.6 alkyl
group, a C.sub.1 -C.sub.6 alkoxy group, or a hydroxyl group),
--L--N(R.sup.8)(R.sup.9) (wherein L, R.sup.8 and R.sup.9 are as
defined above), --L--OR.sup.11 (wherein L is as defined above, and
R.sup.11 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, or a
C.sub.1 -C.sub.6 alkenyl group), --L--OC(O)R.sup.12 (wherein L is
as defined above, and R.sup.12 is a C.sub.1 -C.sub.6 alkyl group or
a C.sub.1 C.sub.6 alkoxy group), --L--S(O).sub.n R.sup.11 (wherein
L, n and R.sup.11 are as defined above), --L--SC(O)R.sup.8 (wherein
L and R.sup.8 are as defined above), ##STR4## (wherein each of L1
and L2 which may be the same or different is a methylene group, an
oxygen atom or a sulfur atom, R.sup.12 is a hydrogen atom or a
C.sub.1 -C.sub.3 alkyl group, and m is 2 or 3); and a salt
thereof.
The present invention also provides a selective herbicidal
composition comprising a herbicidally effective amount of at least
one pyrazole derivative of the formula I as defined above or its
salt and an agricultural carrier or diluent.
Further, the present invention provides a method for selectively
controlling weeds, which comprises applying the pyrazole derivative
of the formula I as defined above or its salt to the locus to be
protected.
Furthermore, the present invention provides a substituted benzene
derivative of the formula: ##STR5## wherein G is a carboxyl group,
a halocarbonyl group or a cyanocarbonyl group, and X, Y, Z, V and W
are as defined above.
Now, the present invention will be described in detail with
reference to the preferred embodiments.
In the compound of the formula I of the present inveniton, A, B, X,
Y, Z and Q are preferably selected from the following substituents,
respectively:
A:Me, Et, n-Pr, i-Pr, CH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 C.tbd.CH,
t-Bu
B:H, Me, Et, n-Pr, i-Pr, Cl, Br, CH.sub.2 Cl, CF.sub.3, OMe, OEt,
OPr-i, SMe, CH.sub.2 OMe, CH.sub.2 SMe, CO.sub.2 Me, CO.sub.2
Et
X:Me, Et, n-Pr, i-Pr, n-Bu, i-Bu, s-Bu, t-Bu, OMe, OEt, OPr-n,
OPr-n, OPr-i, OBu-n, OBu-i, OBU-s, OBu-t, F, Cl, Br, I, NO.sub.2
CN, CH.sub.2 F, CHF.sub.2, CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2
Cl, CCl.sub.3, CHClMe, CH.sub.2 CH.sub.2 Cl, CHClCH.sub.2 Cl,
CH.sub.2 Br, CHBrMe, CH.sub.2 CH.sub.2 Br, CH.sub.2 OMe, CH.sub.2
OEt, CH.sub.2 OPr-n, CH.sub.2 OPr-i, CH.sub.2 OBu-n, CH.sub.2
OBu-i, CH.sub.2 OBu-s, CH.sub.2 OBu-t, CHMeOMe, CHMiOEt, CHMeOPr-n,
CHMeOPr-i, CHMeOBu-n, CHMeOBu-i, CHMeObu-s, CHMeOBu-t, CH.sub.2
CH.sub.2 OMe, CH.sub.2 CH.sub.2 OEt, CH.sub.2 CH.sub.2 OPr-i, Ac,
COEt, COPr-n, COPr-i, COOMe, COOEt, COOPr-i, CONHMe, CONHEt,
CONMe.sub.2, CONEt.sub.2, CONEtMe, OCHF.sub.2, OCF.sub.3, OCH.sub.2
CF.sub.3, SMe, SEt, CH.sub.2 SMe, CH.sub.2 SEt, CHMeSMe,
CHMeSEt
Y: ##STR6## OCHMeCH.dbd.CH.sub.2, OCMe.sub.2 CH.dbd.CH.sub.2,
OCH.sub.2 CMe.dbd.CH.sub.2, OCH.sub.2 CH.dbd.CHMe, OCH.sub.2
CH.dbd.CMe.sub.2, OCH.sub.2 C.tbd.CH, OCHMeC.tbd.CH, OCHMe.sub.2
C.tbd.CH, OCH.sub.2 .tbd.CMe, OCH.sub.2 CH.sub.2 F, OCH.sub.2
CHF.sub.2, OCH.sub.2 CF.sub.3, OCH.sub.2 CH.sub.2 Cl, OCHMeCH.sub.2
Cl, OCH.sub.2 CCl.sub.3, OCH.sub.2 CH.sub.2 CH.sub.2 Cl, OCH.sub.2
CH.sub.2 Br, ##STR7## OCH.sub.2 CCl.dbd.CH.sub.2, OCH.sub.2
CH.sub.2 CH.dbd.CH.sub.2, OCH.sub.2 CCl.dbd.CHCl, OCH.sub.2
CH.sub.2 NO.sub.2, OPh,OPh-Me-2 OPh-Cl-4, OPh-NO.sub.2 -4,
OPH.sub.2 CH.sub.2 OMe, OCH.sub.2 CH.sub.2 OEt, OCH.sub.2 CH.sub.2
OPr-n, OCH.sub.2 CH.sub.2 OPr-i, OCH.sub.2 CH.sub.2 OBu-n,
OCH.sub.2 CH.sub.2 OBu-i, OCH.sub.2 CH.sub.2 Bu-s, OCH.sub.2
CH.sub.2 OBu-t, OCHMeCH.sub.2 OMe, OCH.sub.2 CH.sub.2 OPh,
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe, OCH.sub.2 CH.sub.2 OH,
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe, OCH.sub.2 Ph, OCHMePh,
OCH.sub.2 Ph-4-Me, OCH.sub.2 Ph-4-Cl, OCH.sub.2 CH.sub.2 Ph,
##STR8## OCH.sub.2 CH.sub.2 NH.sub.2, OCH.sub.2 CH.sub.2 NHMe,
OCH.sub.2 CH.sub.2 NMe.sub.2, OCH.sub.2 CH.sub.2 NEt.sub.2,
OCH.sub.2 COOMe, OCH.sub.2 COOEt, OCH.sub.2 COOPr-n, OCH.sub.2
COOPr-i, OCH.sub.2 COOBu-t, OCHMeCOOMe, OCHMeCOOEt OCHMeCOOPr-n,
OCHMeCOOPr-i, OCHMeCOOBu-t OCH.sub.2 CH.sub.2 CN, OCH.sub.2 CN,
OCHMeCN, OCH.sub.2 SMe, OCH.sub.2 C(O)Ph, OCH.sub.2 C(O)Me,
OCH.sub.2 CH.sub.2 SMe, OCH.sub.2 CH.sub.2 SOMe, OCH.sub.2 CH.sub.2
SO.sub.2 Me, OCH.sub.2 CH.sub.2 SEt, OCH.sub.2 CH.sub.2 SO.sub.2
Et, OCOOMe, OCOOEt, OCOOPr-i, OCONH.sub.2, OCONHMe, OCONMe.sub.2,
OP(O)(OMe).sub.2, OP(O)(OEt).sub.2, ##STR9## SCH.sub.2
CH.dbd.CH.sub.2, SCH.sub.2 C.tbd.CH, SCH.sub.2 CF.sub.3, SCH.sub.2
CH.sub.2 Cl, SCH.sub.2 CCl.sub.3, ##STR10## SPh, SCH.sub.2 CH.sub.2
OMe, SCH.sub.2 CH.sub.2 OEt, SCH.sub.2 CH.sub.2 OPr-i, SCH.sub.2
CH.sub.2 OPh, ##STR11## S(O)CH.sub.2 .dbd.CH.sub.2, S(O)CH.sub.2
CH.tbd.CH,S(O)CH.sub.2 CF.sub.3, S(O)CH.sub.2 CH.sub.2 Cl,
##STR12## S(O)Ph, S(O)CH.sub.2 CH.sub.2 OMe, S(O)CH.sub.2 CH.sub.2
OEt, S(O)CH.sub.2 CH.sub.2 OPr-i, S(O)CH.sub.2 CH.sub.2 OPh,
##STR13## SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2, SO.sub.2 CH.sub.2
C.tbd.CH, SO.sub.2 CH.sub.2 CF.sub.3, SO.sub.2 CH.sub.2 CH.sub.2
Cl, SO.sub.2 CH.sub.2 ##STR14## SO.sub.2 Ph, SO.sub.2 CH.sub.2
CH.sub.2 OMe, SO.sub.2 CH.sub.2 CH.sub.2 OEt, SO.sub.2 CH.sub.2
CH.sub.2 OPr-i, Z : F, Cl, Br, I, NO.sub.2, OMe, OEt, OPr-n, OPr-i,
CF.sub.3, CN, SMe, SOMe, SO.sub.2 Me, SCF.sub.3, SOCF.sub.3,
SO.sub.2 CF.sub.3 .
Q : H, Me, Et, n-Pr, i-Pr, n-Bu, i-Bu, s-Bu, t-Bu, CH.sub.2
CH.sub.2 Cl, CH.sub.2 CF.sub.3, CHClMe, CH.sub.2 CH.sub.2 Br,
CHClCH.sub.2 Cl, CH.sub.2 CH.dbd.CH.sub.2, CH.sub.2
CME.dbd.CH.sub.2, CH.sub.2 CH.dbd.CHMe, CH.sub.2 C.tbd.CH, CH.sub.2
CCl.dbd.CH.sub.2, CH.sub.2 CN, CH.sub.2 Ph, CH.sub.2 Ph-Cl-2,
CH.sub.2 Ph-Cl-3, CH.sub.2 Ph-Me-2, ##STR15## CH.sub.2 Ph-Me.sub.2
-2,4, CH.sub.2 Ph-Me-4, CHMePh, CHEtPh, CH.sub.2 Ph-NO.sub.2 -2,
CH.sub.2 Ph-CF.sub.3 -3, CH.sub.2 OMe, CH.sub.2 OEt, CH.sub.2 OH,
CHMeOH, CH.sub.2 NHMe, CH.sub.2 NMe.sub.2, CHMeNM.sub.2, CH.sub.2
COPh, CH.sub.2 COPh-NO.sub.2 -4, CH.sub.2 COPh-Me-4, CH.sub.2
COPh-Cl-4, CH.sub.2 COPh-Me.sub.2 -2,4, CH.sub.2 COPh-CF.sub.3 -4,
CH.sub.2 Ac, CH.sub.2 COEt, CHMeAc, CH.sub.2 CO.sub.2 Me, CH.sub.2
CO.sub.2 Et, CH.sub.2 CO.sub.2 Pr-n, CH.sub.2 CO.sub.2 Pr-i,
CH.sub.2 CO.sub.2 Bu-t, CH.sub.2 CO.sub.2 H, CHMeCO.sub.2 H,
CH.sub.2 CONHMe, CH.sub.2 CONMe.sub.2, CH.sub.2 CONHEt, CH.sub.2
CONEt.sub.2, CH.sub.2 CONPr-n.sub.2, CH.sub.2 OCH.sub.2
CH.dbd.CH.sub.2, CH.sub.2 OAc, CH.sub.2 COEt, CH.sub.2 COPr-i,
CH.sub.2 COBu-t, CH.sub.2 OCO.sub.2 Me, CH.sub.2 OCO.sub.2 Et,
CH.sub.2 OCO.sub.2 Pr-i, CH.sub.2 OCO.sub.2 Bu-t, CH.sub.2 SMe,
CH.sub.2 SEt, CH.sub.2 SCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 SAc,
CH.sub.2 SCOBu-t, CH.sub.2 SO.sub.2 Me, CH.sub.2 SO.sub.2 Et,
CH.sub.2 SO.sub.2 CH.sub.2 CH.dbd.CH.sub.2, CH.sub.2 NHCH.sub.2
CH.dbd.CH.sub.2, CH.sub.2 NMeCH.sub.2 CH.dbd.CH.sub.2, CH.sub.2
NHAc, CH.sub.2 NHCOEt, CH.sub.2 NHCO.sub.2 Me, CH.sub.2 NHCO.sub.2
Et, CH.sub.2 NMeCO.sub.2 Me, COPh, COPh-Me- 4, COPh-NO.sub.2 -2,
COPh-Cl.sub.2 -2,4, Ac, COEt, COPr-n, COPr-i, COBu-n, COBu-t,
COCH.sub.2 Cl, COCHCl.sub.2, COCCl.sub.3, COCF.sub.3, COCH.sub.2
OMe, COCH.sub.2 OPh, COCH.sub.2 CH.dbd.CHCH.sub.3, CO.sub.2 Me,
CO.sub.2 Et, CO.sub.2 Bu-t, CO.sub.2 Pr-i, CONHMe, CONMe.sub.2,
CONHEt, CONEt.sub.2, CONPr-n.sub.2, CON(CH.sub.2
CH.dbd.CH.sub.2).sub.2, CONMePh, ##STR16## CO.sub.2 CH.sub.2 Ph,
CO.sub.2 Ph, SO.sub.2 Me, SO.sub.2 Et, SO.sub.2 CH.sub.2
CH.dbd.CH.sub.2, SO.sub.2 Ph, SO.sub.2 Ph-Me-4, SO.sub.2 Ph-Cl-4,
SO.sub.2 Ph-(NO.sub.2).sub.2 -2,4 SO.sub.2 CF.sub.3,
P(.dbd.O)(OMe).sub.2, P(.dbd.O)(OEt).sub.2, P(.dbd.O)(OPr-n).sub.2,
P(.dbd.O)(OPr-i).sub.2, P(.dbd.S)(OMe).sub.2, P(.dbd.S)(OEt).sub.2,
P(.dbd.O)OMeOPh, P(.dbd.O)(OCH.sub.2 CH.dbd.CH.sub.2).sub.2,
P(.dbd.O)OPhOCH.sub.2 CH.dbd.CH.sub.2
When Q is a hydrogen atom, the compound may readily from a salt
with a metal or with an organic base.
As such a metal, sodium, potassium, calcium, lithium, barium,
magnesium, iron, copper, nickel or manganese may be mentioned.
As such an organic base, methylamine, dimethylamine,
trimethylamine, ethylamine, diethylamine, triethylamine,
n-propylamine, di-n-propylamine, i-propylamine, di-i-propylamine,
n-butylamine, i-butylamine, sec-butylamine, tert-butylamine,
piperidine, pyrrolidine, morpholine, pyridine, N,N-dimethylaniline
or choline may be mentioned.
In the course of researches on the herbicidal properties of various
organic compounds with an aim to develop useful herbicides, the
present inventors have found that the above-mentioned compound of
the present invention exhibits excellent herbicidal activities
against narrow leaf weeds (gramineous and cyperaceous weeds) and
against broad leaf weeds and no substantial phytotoxicity against
useful plants e.g. crop plants such as Zea mays (corn), Sorghum
bicolor (sorgo), Triticum spp (wheat) and Hordeum vulgare (barley).
The present invention has been accomplished on the basis of this
discovery.
The compound of the present invention exhibits strong herbicidal
activities in each of soil treatment, soil incorporation treatment
and foliage treatment. On the other hand, it exhibits no
phytotoxicity against crop plants such as Zea mays, Sorghum
bicolor, Triticum spp and Hordeum vulgare in a practical
application in any of soil treatment, soil incorporation treatment
and foliage treatment. Thus, the compound of the present invention
has high selectivity and it is extremely effective for controlling
weeds during the cultivation of these crop plants. Namely, the
compound of the present invention exhibits strong herbicidal
activities against noxious weeds such as Setaria viridis (green
foxtail), Echinochloa crus-galli (barnyardgrass), Amarathus lividus
(livid amaranth), Polvgonum longisetum (persicaria blumei gross),
Xanthium strumarium (cocklebur), Abutilon theophrasti (velvet leaf)
and Cyperus esculentus (yellow nutsedge), which develop during the
cultivation of Zea mays or Sorphum bicolor. The herbicidal
activities against gramineous weeds and Cyperus esculentus are
remarkablly high and extremely unique. Heretofore, during the
cultivation of Zea mays or Sorghum bicolor, it has been common to
employ atranzine or cyanazine as a triazine-type herbicide, or
alachlor or metolachlor as an acid anilide type herbicide. However,
atranzine and cyanazine have poor herbicidal activities against
gramineous weeds although they show high activities against broad
leaf weeds, and their activities against Cyperus esculentus are
very low. On the other hand, alachlor and metolachlor have poor
activities against broad leaf weeds although their activities
against gramineous weeds are high, and their activities against
Cyperus esculentus are very poor. Thus, it has been difficult to
eradicate all the weed species by a single application of such
herbicides.
As a result of various studies, the present inventors have found
the compound of the present invention which exhibits excellent
herbicidal effects against a wide range of weeds, and the present
invention has been accomplished on the basis of this discovery. The
compound of the present invention also has a feature that it
exhibits no phytotoxicity against crop plants such as Zea mays,
Sorqhum bicolor, Triticum spp and Hordeum vulgare and thus can
safely be applied to the fields for such crop plants.
Further, the compound of the present invention includes a compound
which shows selectivity between Oryza sativa (rice) and Echinochloa
crus-qalli (barnyardgrass), and it also includes a compound having
selectivity for a useful plant such as Goxxypium spp (cotton), Beta
vulgaris (sugar beat) or Clycine max (soybean).
Heretofore, it has been known that 4-benzoylpyrazole derivatives
have excellent herbicidal activities. For example, pyrazolate
(common name) is commercially available and widely used for
practical application. However, such conventional herbicides are
restricted in their application to paddy fields, and their
activities are very poor in their application to upland fields.
Whereas, as a result of extensive research for many years on
4-benzoylpyrazole derivatives, the present inventors have finally
found that the compound of the present invention which
simultaneously satisfies the various conditions for substituents in
the structure as specified above, exhibits strong herbicidal
activities in the application to upland fields in each of soil
treatment, soil incorporation treatment and foliage treatment. It
has been found that the compound of the present invention exhibits
particularly high activities against gramineous weeds and Cyperus
esculentus.
The compound of the present invention can readily be prepared by
any one of the following reactions. ##STR17##
In the above formulas, A, B, V, W, X, Y, Z and Q are as defined
above, E is a halogen atom, a methanesulfonyloxy group or a
p-toluenesulfonyloxy group. Further, ##STR18## and may be
represented by either formula.
Reaction scheme (1) represents a reaction wherein benzoic acid
having suitable substituents and 5-hydroxypyrazole are reacted in
an inert solvent in the presence of a condensation agent and a base
to obtain 4-benzoyl-5-hydroxypyrazole. The condensation agent is
used in an amount of from 1.0 to 1.5 mols per mol of the benzoic
acid and pyrazole. As the condensation agent,
N,N'-dicyclohexylcarbodiimide may be mentioned. The solvent may be
any aolvent so long as it is inert to the reaction. Particularly
preferred is tert-butyl alcohol, tert-amyl alcohol or isopropyl
alcohol. The base may not necessarily be required. However, in
general, the yield can be improved by using a base. There is no
particular restriction as to the base, but potassium carbonate or
sodium carbonate may preferably be employed. The reaction
temperature may range from room temperature to boiling point of the
solvent, but is peferably from 50.degree. to 100.degree. C.
The reaction time is usually from 0.5 to 20 hours.
Reaction scheme (2) shows a reaction wherein benzoyl chloride
having suitable substituents and 5-hydroxypyrazole are reacted to
form a benzoyl ester, which is then rearranged to a 4-benzoyl
compound.
The benzoyl esterification can be accomplished in an inert solvent
(such as an aromatic hydrocarbon, a fatty acid ester, a halogenated
hydrocarbon, an ether, acetonitrile, dimethylsulfoxide or
N,N'-dimethylformamide) or in a two phase system with such a
solvent and water or in a mixture of such solvents in the presence
of a suitable dehydrochlorinating agent (e.g. an inorganic base
such as sodium hydroxide, potassium hydroxide or sodium
hydrogencarbonate, or an organic base such as pyridine or
triethylamine) at a temperature of from room temperature to
100.degree. C. for from 10 minutes to 5 hours.
The rearrangement reaction can be accomplished by means of a Lewis
acid such as anhydrous aluminum chloride or a base. As the base,
potassium carbonate, calcium hydroxide or sodium carbonate may be
used. The Lewis acid or base is used usually in an amount of from 1
to 10 mol times.
No solvent is required. However, in some cases, it is advantageous
to use a solvent having a suitable boiling point to improve the
operation efficiency or the yield. As such an advantageous example,
use of dioxane, toluene or xylene diglyme, may be mentioned.
The reaction temperature is usually from 50.degree. to 150.degree.
C., and the reaction time is usually from 15 minutes to 30
hours.
Reaction scheme (3) shows a reaction wherein a benzene derivative,
a 5-hydroxypyrazole derivative and carbon tetrachloride are
condensed in the presence of a Lewis acid in an inert solvent or in
the absence of a solvent, followed by hydrolysis to obtain a
4-benzoyl-5-hydroxypyrazole derivative. As the Lewis acid,
anhydrous aluminum chloride or anhydrous aluminum bromide in an
amount of at least the theoretical amount for the reaction is
preferred. The solvent may be of any type so long as it is inert to
the reaction. However, a chlorine-type solvent such as methylene
chloride, dichloroethane or tetrachloroethane is preferred. The
temperature for condensation may range from 0.degree. C. to the
boiling point of the solvent, but it is preferably from 10.degree.
to 80.degree. C. The hydrolysis is conducted in the presence of
hydrochloric acid or sulfuric acid. The temperature for the
hydrolysis is preferably from room temperature to 100.degree. C.
The time for the hydrolysis is usually from 0.1 to 10 hours.
Reaction scheme (4) shows a reaction wherein a benzoyl cyanide
derivative and a 5-hydroxypyrazole derivative are reacted in the
presence of a Lewis acid and a base in an inert solvent or in the
absence of a solvent to obtain a 4-benzoyl-5-hydroxypyrazole. As
the Lewis acid, zinc chloride, aluminum chloride or aluminum
bromide may be used. As the base, pyridine or triethylamine may be
mentioned. The Lewis acid and the base are used usually in an
amount of from 1 to 10 mol times. As the solvent, methylene
chloride, dichloroethane or tetrachloroethane may be mentioned. The
reaction temperature is usually from 0.degree. to 80.degree. C.,
preferably from 10.degree. to 50.degree. C. The reaction time is
from 0.5 to 20 hours.
Reaction scheme (5) shows a reaction wherein
4-benzoyl-5-hydroxyyrazole is condensed with a halide, a
methanesulfonic acid ester or a p-toluenesulfonic acid ester.
For this reaction, it is preferred to employ from 1 to 3 mol times
of a dehydrohalogenating agent. As such a dehydrohalogenating
agent, an inorganic base such as sodium hydroxide, potassium
hydroxide, sodium carbonate, sodium hydrogencarbonate or potassium
carbonate, or an organic base such as pyridine or triethylaine, may
be mentioned.
There is no particular restriction as to the solvent so long as it
is inert to the reaction. A wide range of solvents including an
aromatic hydrocarbon, a fatty acid ester, a halogenated
hydrocarbon, an ether, a ketone, an aliphatic hydrocarbon,
acetonitrile, dimethylsulfoxide and dimethylformamide may be
used.
The reaction temperature may be optionally selected within a range
of from room temperature to the boiling point of the solvent. The
reaction time is usually from 30 minutes to 30 hours.
Reaction scheme (6) shows a reaction wherein
4-benzoyl-5-hydroxypyrazole is converted to a 5 halogeno compound
by a halogenating agent, or to a methanesulfonate compound or a
p-toluenesulfonate compound by methane sulfonyl chloride or
p-toluenesulfonyl chloride, followed by condensation with a
suitable alcohol or acid.
As the halogenating agent, phosphorus oxychloride, phosphorus
pentachloride or thionyl chloride may be mentioned.
As the solvent, a wide range of solvents inert to the reaction,
such as dimethylformamide, may be employed. However, the reaction
can be conducted without any solvent.
The reaction temperature is preferably from 30.degree. to
150.degree. C, and the reaction time is usually from 30 minutes to
10 hours. In some cases, the reaction time may be shortened or the
yield may be improved by an addition of a dehydrohalogenating
agent.
The condensation reaction with an alcohol or acid is conducted by
an addition of a dehydrohalogenating agent.
As such a dehydrohalogenating agent, a base such as sodium
hydroxide, potassium hydroxide, sodium carbonate, potassium
carbonate, sodium alkoxide or sodium hydride may be employed.
The solvent may be any solvent which is inert to the reaction (such
as an aromatic hydrocarbon, an ether, a ketone or
N,N'-dimethylformamide). The reaction temperature may be selected
within a range of from room temperature to the boiling point of the
solvent.
The substituted benzene derivatives used as the starting materials
for the compounds of the present invention have novel structures,
and they may readily be prepared by a proper combination of various
known syntheses. For instance, compounds wherein the substituent Z
in the benzene ring is --S(O).sub.n CH.sub.3 can be prepared in
accordance with the following reaction schemes. ##STR19##
In the above formulas, X and Y are as defined above, and Hal is a
halogen atom.
Now, the preparation of the substituted benzene derivatives and
pyrazole derivatives will be described in detail with reference to
Examples. However, it should be understood that the present
invention is by no means restricted by such specific Examples.
EXAMPLE 1
Preparation of
4-(2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoyl)-1-ethyl-5-hydrox
ypyrazole
(1) (2-methoxy)ethyl
2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoate
1.2 g of 2-chloro-3-hydroxy-4-methanesulfonylbenzoic acid, 1.4 g of
potassium carbonate and 2.1 g of 2bromoethyl methyl ether were put
into 20 ml of N,N-dimethylformamide and reacted under heating at a
temperture of from 60.degree. to 70.degree. C. for from 6 to 7
hours. Then, the solvent was distilled off, and after an addition
of water, the reaction mixture was extracted with chloroform. The
extract was dried over anhydrous sodium sulfate, and the solvent
was distilled off to obtain 1.9 g of a crude product of the above
identified compound.
(2) 2 -chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoic acid
1.9 g of the crude product of (2-methoxy)ethyl
2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoate was
dissolved in 50 ml of ethanol, and 20 ml of an aqueous solution
containing 1 g of sodium hydroxide was added thereto. The mixture
was stirred at room temperature for 30 minutes. Then, ethanol was
distilled off, and water was added to the residue. The mixture was
washed with chloroform, then acidified with concentrated
hydrochloric acid and extracted with chloroform. The extract was
dried over anhydrous sodium sulfate. Then, the solvent was
distilled off to obtain 1.4 g of a crude product of the above
identified compound. To the crude product, n-hexane was added, and
the mixture was left to stand, whereby the desired product was
gradually crystallized. Melting point: 89.degree.-92.degree. C.
(3)
4-(2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoyl)-1-ethyl-5-hydrox
ypyrazole
1.2 g of the crude product of
2-chloro-4-methanesulfonyl-3-(2-methoxy)ethoxybenzoic acid, 0.3 g
of potassium carbonate, 0.45 g of 1-ethyl-5-hydroxypyrazole and
0.77 g of N,N'-dicyclohexyl carbodiimide were put into 40 ml of
t-amyl alcohol, and the mixture was stirred under heating at a
temperature of from 80.degree. to 90.degree. C. for from 4 to 5
hours. The solvent was distilled off, and a dilute potassium
carbonate aqueous solution was added to the residue. The mixture
was washed with chloroform. The aqueous layer was acidified with
concentrated hydrochloric acid and extracted with chloroform. The
extract was dried over anhydrous sodium sulfate. Then, the solvent
was distilled off to obtain a crude product of the above identified
compound. The crude product was recrystallized from ethanol to
obtain 0.3 g of the desired product. Melting point:
159.degree.-160.degree. C.
EXAMPLE 2
Preparation of
4-(3-benzyloxy-2-chloro-4-methanesulfonylbenzoyl)-1-ethyl-5-hydroxypyrazol
e (1}Benzyl 3-benzyloxy-2-chloro-4-methanesulfonylbenzoate
1.5 g of 2-chloro-3-hydroxy-4-methanesulfonylbenzoic acid, 1.7 g of
potassium carbonate and 5.1 g of benzyl bromide were put into 50 ml
of dimethylformamide, and the mixture was stirred at room
temperature overnight and then heated at a temperature of from
60.degree. to 70.degree. C. for 3 hours. The solvent was distilled
off, and water was added to the residue. The mixture was extracted
with chloroform. The extract was dried over anhydrous sodium
sulfate. Then, the solvent was distilled off to obtain a crude
product of the above identified compound. The crude product was
recrystallized from ethanol to obtain 2.5 g of the desired
product.
(2) 3-benzyloxy-2-chloro-4-methanesulfonylbenzoic acid
2.5 g of benzyl 3-benzyloxy-2-chloro-4-methanesulfonylbenzoate was
put into 50 ml of ethanol, and 25 ml of an aqueous solution
containing 1 g of sodium hydrochloride was added thereto. The
mixture was stirred at room temperature for 30 minutes. Then,
ethanol was distilled off, and water was added to the residue. The
mixture was washed with chloroform. The aqueous layer was acidified
with concentrated hydrochloric acid and then extracted with
chloroform. The extract was dried over anhydrous sodium sulfate.
Then, the solvent was distilled off to obtain a crude product of
the above identified compound. The crude product was washed with
ethanol-isopropyl ether to obtain 1.0 g of the desired product.
(3)-4-(3-benzyloxy-2-chloro-4-methanesulfonylbenzol)-ethyl-5-hydroxypyrazol
1.0 g of 3-benzyloxy-2-chloro-4methanesulfonylbenzoic acid, 0.23 g
of potassium carbonate, 0.24 g of 1-ethyl-5-hydroxy-pyrazole and
0.59 g of N,N'-dicyclohexylcarbodiimide were put into 20 ml of
t-amyl alcohol, and the mixture was stirred under heating at a
temperature of from 80.degree. to 90.degree. C. for 4 hours. The
solvent was distilled off, and then an aqueous potassium carbonate
solution was added to the residue. The mixture was washed with
chloroform. The aqueous layer was acidified with concentrated
hydrochloric acid and then extracted with chloroform. The extract
was dried over anhydrous sodium sulfate. Then, the solvent was
distilled off to obtain a crude product of the above identified
compound. The crude product was recrystallized from ethanol to
obtain 0.3 g of the desired product. Melting point:
162.degree.-165.degree. C.
The physical properties of the benzoic acids and the pyrazole
derivatives prepared in accordance with the preceeding Examples
will be given in Tables 1 and 2 including those of the preceeding
Examples.
TABLE 1 ______________________________________ ##STR20## Melting X
Y Z point (.degree.C.) ______________________________________ Cl
##STR21## SO.sub.2 Me 102.about.107 Cl OCH.sub.2 CH.sub.2 OPh
SO.sub.2 Me 147.about.151 Cl ##STR22## SO.sub.2 Me 153.about.157 Cl
OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me 90.about.94 Cl OCH.sub.2
CHCHMe SO.sub.2 Me 113.about.118 Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2
Me 89.about.92 ______________________________________
TABLE 2
__________________________________________________________________________
##STR23## Compound Melting No. A B X Y Z Q point (.degree.C.)
__________________________________________________________________________
1 Et H Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H 159.about.160 2 Et H
Cl OCH.sub.2 Ph SO.sub.2 Me H 162.about.165 3 Et H Cl ##STR24##
SO.sub.2 Me H 156.about.159 4 Et H Cl ##STR25## SO.sub.2 Me H
153.about.157 5 Et H Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H
148.about.150 6 Et H Cl OCH.sub.2 CCH SO.sub.2 Me H
150.7.about.152.4 7 Et H Cl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H
152.3.about.154.9 8 Et H Cl OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2
Me H 131.about.134 9 Et H Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H
Oily substance 10 Et H Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2
Me H 206.about.208 11 Et H Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H 171.about.174 12 Et H Cl ##STR26## SO.sub.2 Me H 191.about.193 13
Me Me Cl ##STR27## SO.sub.2 Me H 181.about.183.5 14 Et H Cl
##STR28## SO.sub.2 Me H 100.about.101 15 Et H Cl ##STR29## SO.sub.2
Me H 171.about.173 16 Me Me Cl ##STR30## SO.sub.2 Me H
138.about.142 17 Me Me Cl ##STR31## SO.sub.2 Me H 100.5.about.101
18 Et H Cl ##STR32## SO.sub.2 Me H 154.about.158 19 Et H Cl
##STR33## SO.sub.2 Me H 175.about.179 20 i-Pr H Cl OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me H 180.about.183
__________________________________________________________________________
Compounds which can be prepared in the same manner as the preceding
Examples will be given in Tables 3 to 8 including those of the
preceding Examples. However, the present invention is not
restricted to such compounds.
Various symbols used in Tables 3 to 8 have the following meanings.
##STR34##
TABLE 3 ______________________________________ X Y Z Q
______________________________________ Me Y1 SO.sub.2 Me H Me Y2
SO.sub.2 Me H Me Y3 SO.sub.2 Me H Me Y4 SO.sub.2 Me H Me Y5
SO.sub.2 Me H Me Y6 SO.sub.2 Me H Me Y7 SO.sub.2 Me H Me OCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Me OCHMeCHCH.sub.2 SO.sub.2 Me H Me
OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CMeCH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CHCHMe SO.sub.2 Me H Me OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2
Me H Me OCH.sub.2 CCH SO.sub.2 Me H Me OCHMeC CH SO.sub.2 Me H Me
OCMe.sub.2 CCH SO.sub.2 Me H Me OCH.sub.2 CCMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Me OCH.sub.2 CHF.sub.2 SO.sub.2
Me H Me OCH.sub.2 CF.sub.3 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H Me OCH.sub.2 CCl.sub.3 SO.sub.2 Me H Me OCHMeCH.sub.2
Cl SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H Me Y8 SO.sub.2 Me H Me
OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CClCHCl SO.sub.2
Me H Me OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me H Me OPh SO.sub.2
Me H Me OPhMe-2 SO.sub.2 Me H Me OPhCl-4 SO.sub.2 Me H Me
OPhNO.sub.2 -4 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
H Me OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
OPr-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-i
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H Me OCH.sub.2 CH.sub.2Y4
SO.sub.2 Me H Me OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CHMeOMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 OH SO.sub.2 Me H Me OCH.sub.2 Ph SO.sub.2 Me H Me OCHMePh
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Me OCH.sub.2
Ph-2-Cl SO.sub.2 Me H Me OCH.sub.2 Ph-3-Me SO.sub.2 Me H Me
OCH.sub.2 Ph-4-OMe SO.sub.2 Me H Me OCH.sub.2 Ph-4-NO.sub.2
SO.sub.2 Me H Me Y9 SO.sub.2 Me H Me Y10 SO.sub.2 Me H Me Y11
SO.sub.2 Me H Me Y12 SO.sub.2 Me H Me Y13 SO.sub.2 Me H Me Y14
SO.sub.2 Me H Me Y15 SO.sub.2 Me H Me Y16 SO.sub.2 Me H Me Y17
SO.sub.2 Me H Me Y18 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 NHPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NME.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Me Y19
SO.sub.2 Me H Me OCH.sub.2 COOMe SO.sub.2 Me H Me OCH.sub.2 COOEt
SO.sub.2 Me H Me OCH.sub.2 COOPr-i SO.sub.2 Me H Me OCH.sub.2
COOBu-i SO.sub.2 Me H Me OCH.sub.2 COOBu-t SO.sub.2 Me H Me
OCH.sub.2 COOY4 SO.sub.2 Me H Me OCHMeCOOMe SO.sub.2 Me H Me
OCHMeCOOEt SO.sub.2 Me H Me OCHMeCOOPr-i SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H Me OCH.sub.2 SMe SO.sub. 2 Me H Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 S(O)Me
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
S(O)Pr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me H Me OCOOMe SO.sub.2 Me H Me OCOOPr-i SO.sub.2 Me H Me
OCONH.sub.2 SO.sub.2 Me H Me OCONHMe SO.sub.2 Me H Me OCONMe.sub.2
SO.sub.2 Me H Me OP(O)(OMe).sub.2 SO.sub.2 Me H Me Y20 SO.sub.2 Me
H Me SCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H Me SCH.sub.2 CCH SO.sub.2 Me H Me SCH.sub.2 CF.sub.3
SO.sub.2 Me H Me SCH.sub.2 CCl.sub.3 SO.sub.2 Me
H Me Y21 SO.sub.2 Me H Me SPh SO.sub.2 Me H Me SCH.sub.2 CH.sub.2
OMe SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me Y22 SO.sub.2 Me H Me
S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me S(O)CH.sub.2 CHCMe.sub.2
SO.sub.2 Me H Me S(O)CH.sub.2 CCH SO.sub.2 Me H Me S(O)CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Me Y23 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CHCH.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2
Me H Me SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CF.sub.3 SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me
H Me Y24 SO.sub.2 Me H Me Y25 SO.sub.2 Me H Me SO.sub.2 Ph SO.sub.2
Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me SO.sub.2
CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2
OPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub. 2
Ph Me OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me OCHMeCH.sub.2 OMe
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Me
OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2
S(O)Pr-i SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2
Pr-i SO.sub.2 Me CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me
SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
Me OCH.sub. 2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2
OEt Cl H Me OCH.sub.2 CH.sub.2 OPr-i Cl H Me OCHMeCH.sub.2 OMe Cl H
Me OCH.sub.2 COOMe Cl H Me OCH.sub.2 CH.sub.2 SMe Cl H Me OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Me SCH.sub.2 CH.sub.2 OMe Cl H Me
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh Me
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh Me SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2
COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl Y1
SO.sub.2 Me H Cl Y2 SO.sub.2 Me H Cl Y3 SO.sub.2 Me H Cl Y4
SO.sub.2 Me H Cl Y5 SO.sub.2 Me H Cl Y6 SO.sub.2 Me H Cl Y7
SO.sub.2 Me H Cl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
OCHMeCHCH.sub.2 SO.sub.2 Me H Cl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me
H Cl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CHCHMe
SO.sub.2 Me H Cl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CCH SO.sub.2 Me H Cl
OCHMeCCH SO.sub.2 Me H Cl OCMe.sub.2 CCH SO.sub.2 Me H Cl OCH.sub.2
CCMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Cl
OCH.sub.2 CHF.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CF.sub.3 SO.sub.2 Me
H Cl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CCl.sub.3
SO.sub.2 Me H Cl OCHMeCH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 Br
SO.sub.2 Me H Cl Y8 SO.sub.2 Me H Cl OCH.sub.2 CClCH.sub.2 SO.sub.2
Me H Cl OCH.sub.2 CClCHCl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
NO.sub.2 SO.sub.2 Me H Cl OPh SO.sub.2 Me H Cl OPhMe-2 SO.sub.2 Me
H Cl OPhCl-4 SO.sub.2 Me
H Cl OPhNO.sub.2 -4 SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 OPr-n SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 OBu-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-s SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2Y4 SO.sub.2 Me H Cl OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl
OCH.sub.2 CHMeOMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 OH SO.sub.2 Me H Cl OCH.sub.2 Ph SO.sub.2 Me H Cl OCHMePh
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Cl OCH.sub.2
Ph-2-Cl SO.sub.2 Me H Cl OCH.sub.2 Ph-3-Me SO.sub.2 Me H Cl
OCH.sub.2 Ph-4-OMe SO.sub.2 Me H Cl OCH.sub.2 Ph-4-NO.sub.2
SO.sub.2 Me H Cl Y9 SO.sub.2 Me H Cl Y10 SO.sub.2 Me H Cl Y11
SO.sub.2 Me H Cl Y12 SO.sub.2 Me H Cl Y13 SO.sub.2 Me H Cl Y14
SO.sub.2 Me H Cl Y15 SO.sub.2 Me H Cl Y16 SO.sub.2 Me H Cl Y17
SO.sub.2 Me H Cl Y18 SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NH.sub.2
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 NHPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NMe.sub.2
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Cl Y19
SO.sub.2 Me H Cl OCH.sub.2 COOMe SO.sub.2 Me H Cl OCH.sub.2 COOEt
SO.sub.2 Me H Cl OCH.sub.2 COOPr-i SO.sub.2 Me H Cl OCH.sub.2
COOBu-i SO.sub.2 Me H Cl OCH.sub.2 COOBu-t SO.sub.2 Me H Cl
OCH.sub.2 COOY4 SO.sub.2 Me H Cl OCHMeCOOMe SO.sub.2 Me H Cl
OCHMeCOOEt SO.sub.2 Me H Cl OCHMeCOOPr-i SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H Cl OCH.sub.2 SMe SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 S(O)Me
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
S(O)Pr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me H Cl OCOOMe SO.sub.2 Me H Cl OCOOPr-i SO.sub.2 Me H Cl
OCONH.sub.2 SO.sub.2 Me H Cl OCONHMe SO.sub.2 Me H Cl OCONMe.sub.2
SO.sub.2 Me H Cl OP(O)(OMe).sub.2 SO.sub.2 Me H Cl Y20 SO.sub.2 Me
H Cl SCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H Cl SCH.sub.2 CCH SO.sub.2 Me H Cl SCH.sub.2 CF.sub.3
SO.sub.2 Me H Cl SCH.sub.2 CCl.sub.3 SO.sub.2 Me H Cl Y21 SO.sub.2
Me H Cl SPh SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H
Cl SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me H Cl Y22 SO.sub.2 Me H Cl S(O)CH.sub.2 CHCH.sub.2
SO.sub.2 Me H Cl S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl
S(O)CH.sub.2 CCH SO.sub.2 Me H Cl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2
Me H Cl Y23 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2
Me H Cl SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl SO.sub.2
CH.sub.2 CCH SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2
Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl Y24 SO.sub.2
Me H Cl Y25 SO.sub.2 Me H Cl SO.sub. 2 Ph SO.sub.2 Me H Cl SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2
OEt SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H
Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 OEt SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 Ph Cl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2
Ph Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph
Cl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 Ph Cl SCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl SCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 Ph Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2
Me CH.sub. 2 Ph Cl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh Cl
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2
CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SOMe
SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me
SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me
CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 COPh Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh
Cl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh Cl SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh Cl SO.sub.2
CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2
CH.sub.2 OMe Cl H Cl OCH.sub.2 CH.sub.2 OEt Cl H Cl OCH.sub.2
CH.sub.2 OPr-i Cl H Cl OCHMeCH.sub.2 OMe Cl H Cl OCH.sub.2 COOMe Cl
H Cl OCH.sub.2 CH.sub.2 SMe Cl H Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me
Cl H Cl SCH.sub.2 CH.sub.2 OMe Cl H Cl SO.sub.2 CH.sub.2 CH.sub.2
OMe Cl H Cl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 SMe Cl CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2
Ph Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph Cl SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 Ph Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl OCH.sub.2
CH.sub.2 SMe Cl CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 COPh Cl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl
SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPh Cl SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh OMe Y1 SO.sub.2 Me H OMe Y2 SO.sub.2
Me H OMe Y3 SO.sub.2 Me H OMe Y4 SO.sub.2 Me H OMe Y5 SO.sub.2
Me
H OMe Y6 SO.sub.2 Me H OMe Y7 SO.sub.2 Me H OMe OCH.sub. 2
CHCH.sub.2 SO.sub.2 Me H OMe OCHMeCHCH.sub.2 SO.sub.2 Me H OMe
OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CMeCH.sub.2
SO.sub.2 Me H OMe OCH.sub.2 CHCHMe SO.sub.2 Me H OMe OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 CHCH.sub.2
SO.sub.2 Me H OMe OCH.sub.2 CCH SO.sub.2 Me H OMe OCHMeCCH SO.sub.2
Me H OMe OCMe.sub.2 CCH SO.sub.2 Me H OMe OCH.sub.2 CCMe SO.sub.2
Me H OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me H OMe OCH.sub.2 CHF.sub.2
SO.sub.2 Me H OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 Cl SO.sub.2 Me H OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe
OCHMeCH.sub.2 Cl SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H OMe Y8
SO.sub.2 Me H OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2
CClCHCl SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me H
OMe OPh SO.sub.2 Me H OMe OPhMe-2 SO.sub.2 Me H OMe OPhCl-4
SO.sub.2 Me H OMe OPhNO.sub.2 -4 SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H
OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
OPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-s
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 -Y4 SO.sub.2 Me H OMe OCHMeCH.sub.2 OMe SO.sub.2
Me H OMe OCH.sub.2 CHMeOMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OPh
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me
H OMe OCH.sub.2 CH.sub.2 OH SO.sub.2 Me H OMe OCH.sub.2 Ph SO.sub.2
Me H OMe OCHMePh SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 Ph SO.sub.2
Me H OMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me H OMe OCH.sub.2 Ph-3-Me
SO.sub.2 Me H OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me H OMe OCH.sub.2
Ph-4-NO.sub.2 SO.sub.2 Me H OMe Y9 SO.sub.2 Me H OMe Y10 SO.sub.2
Me H OMe Y11 SO.sub.2 Me H OMe Y12 SO.sub.2 Me H OMe Y13 SO.sub.2
Me H OMe Y14 SO.sub.2 Me H OMe Y15 SO.sub.2 Me H OMe Y16 SO.sub.2
Me H OMe Y17 SO.sub.2 Me H OMe Y18 SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 NH.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NHMe
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
NEt.sub.2 SO.sub.2 Me H OMe Y19 SO.sub.2 Me H OMe OCH.sub.2 COOMe
SO.sub.2 Me H OMe OCH.sub.2 COOEt SO.sub.2 Me H OMe OCH.sub.2
COOPr-i SO.sub.2 Me H OMe OCH.sub.2 COOBu-i SO.sub.2 Me H OMe
OCH.sub.2 COOBu-t SO.sub.2 Me H OMe OCH.sub.2 COO-Y4 SO.sub.2 Me H
OMe OCHMeCOOMe SO.sub.2 Me H OMe OCHMeCOOEt SO.sub.2 Me H OMe
OCHMeCOOPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 CN SO.sub.2 Me H
OMe OCH.sub.2 SMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2
Me H OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H OMe OCOOMe SO.sub.2
Me H OMe OCOOPr-i SO.sub.2 Me H OMe OCONH.sub.2 SO.sub.2 Me H OMe
OCONHMe SO.sub.2 Me H OMe OCONMe.sub.2 SO.sub.2 Me H OMe
OP(O)(OMe).sub.2 SO.sub.2 Me H OMe Y20 SO.sub.2 Me H OMe SCH.sub.2
CHCH.sub.2 SO.sub.2 Me H OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H
OMe SCH.sub.2 CCH SO.sub.2 Me H OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me
H OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe Y21 SO.sub.2 Me H OMe
SPh SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H OMe
SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me
H OMe Y22 SO.sub.2 Me H OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H
OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H OMe S(O)CH.sub.2 CCH
SO.sub.2 Me H OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H OMe Y23
SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe
SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H OMe SO.sub.2 CH.sub. 2
CCH SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H OMe
SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H OMe Y24 SO.sub.2 Me H
OMe Y25 SO.sub.2 Me H OMe SO.sub.2 Ph SO.sub.2 Me H OMe SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CH.sub.2
OEt SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2
CH.sub.2 OEt SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 Ph OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2
Ph OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph OMe SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 OMe Cl H OMe OCH.sub.2
CH.sub.2 OEt Cl H OMe OCH.sub.2 CH.sub.2 OPr-i Cl H OMe
OCHMeCH.sub.2 OMe Cl H OMe OCH.sub.2 COOMe Cl H OMe OCH.sub.2
CH.sub.2 SMe Cl H OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H OMe
SCH.sub.2 CH.sub.2 OMe Cl H OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H
OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2
SMe Cl CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 Ph OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph OMe SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 Ph OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh OMe
OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2
SO.sub.2 Me Cl CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2
COPh OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPh OMe SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe Y1 SO.sub.2 Me
H CH.sub.2 OMe Y2 SO.sub.2 Me H CH.sub.2 OMe Y3 SO.sub.2 Me H
CH.sub.2 OMe Y4 SO.sub.2 Me H CH.sub.2 OMe Y5 SO.sub.2 Me H
CH.sub.2 OMe Y6 SO.sub.2 Me H CH.sub.2 OMe Y7 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
OCHMeCHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCMe.sub.2 CHCH.sub.2
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CCH SO.sub.2 Me H
CH.sub.2 OMe OCHMeCCH SO.sub.2 Me H CH.sub.2 OMe OCMe.sub.2 C CH
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CHF.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me
H CH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CCl.sub.3 SO.sub.2 Me H CH.sub.2 OMe OCHMeCH.sub.2 Cl
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2
Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H CH.sub.2 OMe
Y8 SO.sub.2 Me
H CH.sub.2 OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CClCHCl SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
NO.sub.2 SO.sub.2 Me H CH.sub.2 OMe OPh SO.sub.2 Me H CH.sub.2 OMe
OPhMe-2 SO.sub.2 Me H CH.sub.2 OMe OPhCl-4 SO.sub.2 Me H CH.sub.2
OMe OPhNO.sub.2 -4 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
OMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OBu-n SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 -Y4 SO.sub.2 Me H CH.sub.2 OMe OCHMeCH.sub.2 OMe
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CHMeOMe SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OH SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph
SO.sub.2 Me H CH.sub.2 OMe OCHMePh SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph-2-Cl
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
Ph-4-NO.sub.2 SO.sub.2 Me H CH.sub.2 OMe Y9 SO.sub.2 Me H CH.sub.2
OMe Y10 SO.sub.2 Me H CH.sub.2 OMe Y11 SO.sub.2 Me H CH.sub.2 OMe
Y12 SO.sub.2 Me H CH.sub.2 OMe Y13 SO.sub.2 Me H CH.sub.2 OMe Y14
SO.sub.2 Me H CH.sub.2 OMe Y15 SO.sub.2 Me H CH.sub.2 OMe Y16
SO.sub.2 Me H CH.sub.2 OMe Y17 SO.sub.2 Me H CH.sub.2 OMe Y18
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me
H CH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 NMe.sub.2 SO.sub.2 Me H CH.sub. 2 OMe OCH.sub.2 CH.sub.2
NEt.sub.2 SO.sub.2 Me H CH.sub.2 OMe Y19 SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 COOMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2
Me H CH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 COOBu-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOBu-t
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COO-Y4 SO.sub.2 Me H CH.sub.2
OMe OCHMeCOOMe SO.sub.2 Me H CH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me H
CH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
SPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i
SO.sub.2 Me H CH.sub.2 OMe OCOOMe SO.sub.2 Me H CH.sub.2 OMe
OCOOPr-i SO.sub.2 Me H CH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me H
CH.sub.2 OMe OCONHMe SO.sub.2 Me H CH.sub.2 OMe OCONMe.sub.2
SO.sub.2 Me H CH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me H CH.sub.2
OMe Y20 SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me
H CH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe
SCH.sub.2 CCH SO.sub.2 Me
H CH.sub.2 OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me H CH.sub.2 OMe
SCH.sub.2 CCl.sub.3 SO.sub.2 Me H CH.sub.2 OMe Y21 SO.sub.2 Me H
CH.sub.2 OMe SPh SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H
CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe
Y22 SO.sub.2 Me H CH.sub.2 OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me
H CH.sub. 2 OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe
S(O)CH.sub.2 CCH SO.sub.2 Me H CH.sub.2 OMe S(O)CH.sub.2 CH.sub.2
Cl SO.sub.2 Me H CH.sub.2 OMe Y23 SO.sub.2 Me H CH.sub.2 OMe
SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe SO.sub.2
CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2
CCH SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2
Me H CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H
CH.sub.2 OMe Y24 SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me
H CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H
CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H CH.sub.2
OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub. 2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2
OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2
OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh CH.sub.2
OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh CH.sub.2
OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe
SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh CH.sub.2
OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh
CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OEt Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i Cl H
CH.sub.2 OMe OCHMeCH.sub.2 OMe Cl H CH.sub.2 OMe OCH.sub.2 COOMe Cl
H CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl H CH.sub.2 OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl H
CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2
CH.sub.2 SMe Cl CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe Cl
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2
Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph CH.sub.2 OMe
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2
CH.sub.2 SMe Cl CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2
SO.sub.2 Me Cl CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPh
CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh
______________________________________
TABLE 4 ______________________________________ ; - ##STR35## X Y Z
Q ______________________________________ Me Y1 SO.sub.2 Me H Me Y2
SO.sub.2 Me H Me Y3 SO.sub.2 Me H Me Y4 SO.sub.2 Me H Me Y5
SO.sub.2 Me H Me Y6 SO.sub.2 Me H Me Y7 SO.sub.2 Me H Me OCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Me OCHMeCHCH.sub.2 SO.sub.2 Me H Me
OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CMeCH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CHCHMe SO.sub.2 Me H Me OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2
Me H Me OCH.sub.2 CCH SO.sub.2 Me H Me OCHMeC CH SO.sub.2 Me H Me
OCMe.sub.2 CCH SO.sub.2 Me H Me OCH.sub.2 CCMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Me OCH.sub.2 CHF.sub.2 SO.sub.2
Me H Me OCH.sub.2 CF.sub.3 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H Me OCH.sub.2 CCl.sub.3 SO.sub.2 Me H Me OCHMeCH.sub.2
Cl SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H Me Y8 SO.sub.2 Me H Me
OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CClCHCl SO.sub.2
Me H Me OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me H Me OPh SO.sub.2
Me H Me OPhMe-2 SO.sub.2 Me H Me OPhCl-4 SO.sub.2 Me H Me
OPhNO.sub.2 -4 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
H Me OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
OPr-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-i
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H Me OCH.sub.2 CH.sub.2Y4
SO.sub.2 Me H Me OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CHMeOMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 OH SO.sub.2 Me H Me OCH.sub.2 Ph SO.sub.2 Me H Me OCHMePh
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Me OCH.sub.2
Ph-2-Cl SO.sub.2 Me H Me OCH.sub.2 Ph-3-Me SO.sub.2 Me H Me
OCH.sub.2 Ph-4-OMe SO.sub.2 Me H Me OCH.sub.2 Ph-4-NO.sub.2
SO.sub.2 Me H Me Y9 SO.sub.2 Me H Me Y10 SO.sub.2 Me H Me Y11
SO.sub.2 Me H Me Y12 SO.sub.2 Me H Me Y13 SO.sub.2 Me H Me Y14
SO.sub.2 Me H Me Y15 SO.sub.2 Me H Me Y16 SO.sub.2 Me H Me Y17
SO.sub.2 Me H Me Y18 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 NHPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NMe.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Me Y19
SO.sub.2 Me H Me OCH.sub.2 COOMe SO.sub.2 Me H Me OCH.sub.2 COOEt
SO.sub.2 Me H Me OCH.sub.2 COOPr-i SO.sub.2 Me H Me OCH.sub.2
COOBu-i SO.sub.2 Me H Me OCH.sub.2 COOBu-t SO.sub.2 Me H Me
OCH.sub.2 COOY4 SO.sub.2 Me H Me OCHMeCOOMe SO.sub.2 Me H Me
OCHMeCOOEt SO.sub.2 Me H Me OCHMeCOOPr-i SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H Me OCH.sub.2 SMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 S(O)Me
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
S(O)Pr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me H Me OCOOMe SO.sub.2 Me H Me OCOOPr-i SO.sub.2 Me H Me
OCONH.sub.2 SO.sub.2 Me H Me OCONHMe SO.sub.2 Me H Me OCONMe.sub.2
SO.sub.2 Me H Me OP(O)(OMe).sub.2 SO.sub.2 Me H Me Y20 SO.sub.2 Me
H Me SCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H Me SCH.sub.2 CCH SO.sub.2 Me H Me SCH.sub.2 CF.sub.3
SO.sub.2 Me H
Me SCH.sub.2 CCl.sub.3 SO.sub.2 Me H Me Y21 SO.sub.2 Me H Me SPh
SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me SCH.sub.2
CH.sub.2 OEt SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H Me Y22 SO.sub.2 Me H Me S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Me S(O)CH.sub.2 CCH SO.sub.2
Me H Me S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me Y23 SO.sub.2 Me H
Me SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Me Y24 SO.sub.2 Me H Me Y25 SO.sub.2 Me H
Me SO.sub.2 Ph SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub. 2 Me H Me OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph Me OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
Me OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2
OEt Cl H Me OCH.sub.2 CH.sub.2 OPr-i Cl H Me OCHMeCH.sub.2 OMe Cl H
Me OCH.sub.2 COOMe Cl H Me OCH.sub.2 CH.sub.2 SMe Cl H Me OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Me SCH.sub.2 CH.sub.2 OMe Cl H Me
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh Me
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh Me SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2
COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl Y1
SO.sub.2 Me H Cl Y2 SO.sub.2 Me H Cl Y3 SO.sub.2 Me H Cl Y4
SO.sub.2 Me H Cl Y5 SO.sub.2 Me H Cl Y6 SO.sub.2 Me H Cl Y7
SO.sub.2 Me H Cl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
OCHMeCHCH.sub.2 SO.sub.2 Me H Cl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me
H Cl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CHCHMe
SO.sub.2 Me H Cl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CCH SO.sub.2 Me H Cl
OCHMeCCH SO.sub.2 Me H Cl OCMe.sub.2 CCH SO.sub.2 Me H Cl OCH.sub.2
CCMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Cl
OCH.sub.2 CHF.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CF.sub.3 SO.sub.2 Me
H Cl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CCl.sub.3
SO.sub.2 Me H Cl OCHMeCH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 Br
SO.sub.2 Me H Cl Y8 SO.sub.2 Me H Cl OCH.sub.2 CClCH.sub.2 SO.sub.2
Me H Cl OCH.sub.2 CClCHCl SO.sub.2 Me H Cl OCH.sub. 2 CH.sub.2
NO.sub.2 SO.sub.2 Me H Cl OPh SO.sub.2 Me H Cl OPhMe-2 SO.sub.2
Me
H Cl OPhCl-4 SO.sub.2 Me H Cl OPhNO.sub.2 -4 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-n
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-t
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me H Cl
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CHMeOMe SO.sub.2 Me H
Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OH SO.sub.2
Me H Cl OCH.sub.2 Ph SO.sub.2 Me H Cl OCHMePh SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Cl OCH.sub.2 Ph-2-Cl SO.sub.2
Me H Cl OCH.sub.2 Ph-3-Me SO.sub.2 Me H Cl OCH.sub.2 Ph-4-OMe
SO.sub.2 Me H Cl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me H Cl Y9
SO.sub.2 Me H Cl Y10 SO.sub.2 Me H Cl Y11 SO.sub.2 Me H Cl Y12
SO.sub.2 Me H Cl Y13 SO.sub.2 Me H Cl Y14 SO.sub.2 Me H Cl Y15
SO.sub.2 Me H Cl Y16 SO.sub.2 Me H Cl Y17 SO.sub.2 Me H Cl Y18
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NHPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Cl Y19 SO.sub.2 Me H Cl
OCH.sub.2 COOMe SO.sub.2 Me H Cl OCH.sub.2 COOEt SO.sub.2 Me H Cl
OCH.sub.2 COOPr-i SO.sub.2 Me H Cl OCH.sub.2 COOBu-i SO.sub.2 Me H
Cl OCH.sub.2 COOBu-t SO.sub.2 Me H Cl OCH.sub.2 COOY4 SO.sub.2 Me H
Cl OCHMeCOOMe SO.sub.2 Me H Cl OCHMeCOOEt SO.sub.2 Me H Cl
OCHMeCOOPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me H
Cl OCH.sub.2 SMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H Cl OCOOMe SO.sub.2
Me H Cl OCOOPr-i SO.sub.2 Me H Cl OCONH.sub.2 SO.sub.2 Me H Cl
OCONHMe SO.sub.2 Me H Cl OCONMe.sub.2 SO.sub.2 Me H Cl
OP(O)(OMe).sub.2 SO.sub.2 Me H Cl Y20 SO.sub.2 Me H Cl SCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Cl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl
SCH.sub.2 C CH SO.sub.2 Me H Cl SCH.sub.2 CF.sub.3 SO.sub.2 Me H Cl
SCH.sub.2 CCl.sub.3 SO.sub.2 Me H Cl Y21 SO.sub.2 Me H Cl SPh
SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl SCH.sub.2
CH.sub.2 OEt SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H Cl Y22 SO.sub.2 Me H Cl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl S(O)CH.sub.2 CCH SO.sub.2
Me H Cl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl Y23 SO.sub.2 Me H
Cl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Cl Y24 SO.sub.2 Me H Cl Y25 SO.sub.2 Me H
Cl SO.sub.2 Ph SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph Cl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SPr-i
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CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Cl SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
Cl OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh Cl SCH.sub.2 CH.sub.2 OMe
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CH.sub.2 COPh Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Cl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 OMe Cl H Cl OCH.sub.2 CH.sub.2
OEt Cl H Cl OCH.sub.2 CH.sub.2 OPr-i Cl H Cl OCHMeCH.sub.2 OMe Cl H
Cl OCH.sub.2 COOMe Cl H Cl OCH.sub.2 CH.sub.2 SMe Cl H Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Cl SCH.sub.2 CH.sub.2 OMe Cl H Cl
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H Cl OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 Ph Cl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Cl SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh Cl
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph Cl SCH.sub.2 CH.sub.2
OMe Cl CH.sub.2 COPh Cl SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPh Cl
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh OMe Y1 SO.sub.2 Me
H OMe Y2 SO.sub.2 Me H OMe Y3 SO.sub.2 Me H OMe Y4 SO.sub.2 Me
H OMe Y5 SO.sub.2 Me H OMe Y6 SO.sub.2 Me H OMe Y7 SO.sub.2 Me H
OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe OCHMeCHCH.sub.2 SO.sub.2
Me H OMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2
CMeCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CHCHMe SO.sub.2 Me H OMe
OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
CHCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CCH SO.sub.2 Me H OMe
OCHMeCCH SO.sub.2 Me H OMe OCMe.sub.2 CCH SO.sub.2 Me H OMe
OCH.sub.2 CCMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me H
OMe OCH.sub.2 CHF.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CF.sub.3
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H OMe OCH.sub.2
CCl.sub.3 SO.sub.2 Me H OMe OCHMeCH.sub.2 Cl SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
Br SO.sub.2 Me H OMe Y8 SO.sub.2 Me H OMe OCH.sub.2 CClCH.sub.2
SO.sub.2 Me H OMe OCH.sub.2 CClCHCl SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 NO.sub.2 SO.sub.2 Me H OMe OPh SO.sub.2 Me H OMe OPhMe-2
SO.sub.2 Me H OMe OPhCl-4 SO.sub.2 Me H OMe OPhNO.sub.2 -4 SO.sub.2
Me H OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 OEt SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me
H OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
OBu-n SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-t
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me H OMe
OCHMeCH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CHMeOMe SO.sub.2 Me H
OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
OCHMeCH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OH SO.sub.2
Me H OMe OCH.sub.2 Ph SO.sub.2 Me H OMe OCHMePh SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H OMe OCH.sub.2 Ph-2-Cl SO.sub.2
Me H OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me H OMe OCH.sub.2 Ph-4-OMe
SO.sub.2 Me H OMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me H OMe Y9
SO.sub.2 Me H OMe Y10 SO.sub.2 Me H OMe Y11 SO.sub.2 Me H OMe Y12
SO.sub.2 Me H OMe Y13 SO.sub.2 Me H OMe Y14 SO.sub.2 Me H OMe Y15
SO.sub.2 Me H OMe Y16 SO.sub.2 Me H OMe Y17 SO.sub.2 Me H OMe Y18
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NHPr-i
SO.sub. 2 Me H OMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H OMe Y19 SO.sub.2 Me H
OMe OCH.sub.2 COOMe SO.sub.2 Me H OMe OCH.sub.2 COOEt SO.sub.2 Me H
OMe OCH.sub.2 COOPr-i SO.sub.2 Me H OMe OCH.sub.2 COOBu-i SO.sub.2
Me H OMe OCH.sub.2 COOBu-t SO.sub.2 Me H OMe OCH.sub.2 COOY4
SO.sub.2 Me H OMe OCHMeCOOMe SO.sub.2 Me H OMe OCHMeCOOEt SO.sub.2
Me H OMe OCHMeCOOPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 CN
SO.sub.2 Me H OMe OCH.sub.2 SMe SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 SMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2
Me H OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 S(O)Pr-i
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H
OMe OCOOMe SO.sub.2 Me H OMe OCOOPr-i SO.sub.2 Me H OMe OCONH.sub.2
SO.sub.2 Me H OMe OCONHMe SO.sub.2 Me H OMe OCONMe.sub.2 SO.sub.2
Me H OMe OP(O)(OMe).sub.2 SO.sub.2 Me H OMe Y20 SO.sub.2 Me H OMe
SCH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H OMe SCH.sub.2 CCH SO.sub.2 Me H OMe SCH.sub.2
CF.sub.3 SO.sub.2 Me H OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe
Y21 SO.sub.2 Me H OMe SPh SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H
OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H OMe Y22 SO.sub.2 Me H
OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe S(O)CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H OMe S(O)CH.sub.2 CCH SO.sub.2 Me H OMe
S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H OMe Y23 SO.sub.2 Me H OMe
SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe SO.sub.2 CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H
OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H OMe SO.sub.2 CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H OMe Y24 SO.sub.2 Me H OMe Y25 SO.sub.2 Me
H OMe SO.sub.2 Ph SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H OMe
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub. 2 Ph OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2
Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph OMe SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 OMe Cl H OMe OCH.sub.2
CH.sub.2 OEt Cl H OMe OCH.sub.2 CH.sub.2 OPr-i Cl H OMe
OCHMeCH.sub.2 OMe Cl H OMe OCH.sub.2 COOMe Cl H OMe OCH.sub.2
CH.sub.2 SMe Cl H OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H OMe
SCH.sub.2 CH.sub.2 OMe Cl H OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H
OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2
SMe Cl CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 Ph OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph OMe SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 Ph OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh OMe
OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2
SO.sub.2 Me Cl CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2
COPh OMe SCH.sub. 2 CH.sub.2 OEt Cl CH.sub.2 COPh OMe SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe Y1 SO.sub.2 Me
H CH.sub.2 OMe Y2 SO.sub.2 Me H CH.sub.2 OMe Y3 SO.sub.2 Me H
CH.sub.2 OMe Y4 SO.sub.2 Me H CH.sub.2 OMe Y5 SO.sub.2 Me H
CH.sub.2 OMe Y6 SO.sub.2 Me H CH.sub.2 OMe Y7 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
OCHMeCHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCMe.sub.2 CHCH.sub.2
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CCH SO.sub.2 Me H
CH.sub.2 OMe OCHMeCCH SO.sub.2 Me H CH.sub.2 OMe OCMe.sub.2 CCH
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CHF.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me
H CH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CCl.sub.3 SO.sub.2 Me H CH.sub.2 OMe OCHMeCH.sub.2 Cl
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2
Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H
CH.sub.2 OMe Y8 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CClCH.sub.2
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CClCHCl SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me H CH.sub.2 OMe OPh
SO.sub.2 Me H CH.sub.2 OMe OPhMe-2 SO.sub.2 Me H CH.sub.2 OMe
OPhCl-4 SO.sub.2 Me H CH.sub.2 OMe OPhNO.sub.2 -4 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OPr-n SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OBu-t SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 Y4
SO.sub.2 Me H CH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CHMeOMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
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CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OH SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph SO.sub.2 Me H
CH.sub.2 OMe OCHMePh SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
Ph SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph-2-Cl SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
Ph-4-OMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph-4-NO.sub.2
SO.sub.2 Me H CH.sub.2 OMe Y9 SO.sub.2 Me H CH.sub.2 OMe Y10
SO.sub.2 Me H CH.sub.2 OMe Y11 SO.sub.2 Me H CH.sub.2 OMe Y12
SO.sub.2 Me H CH.sub.2 OMe Y13 SO.sub.2 Me H CH.sub.2 OMe Y14
SO.sub.2 Me H CH.sub.2 OMe Y15 SO.sub.2 Me H CH.sub.2 OMe Y16
SO.sub.2 Me H CH.sub.2 OMe Y17 SO.sub.2 Me H CH.sub.2 OMe Y18
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me
H CH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 NMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
NEt.sub.2 SO.sub.2 Me H CH.sub.2 OMe Y19 SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 COOMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2
Me H CH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 COOBu-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOBu-t
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOY4 SO.sub.2 Me H CH.sub.2
OMe OCHMeCOOMe SO.sub.2 Me H CH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me H
CH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
SPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i
SO.sub.2 Me H CH.sub.2 OMe OCOOMe SO.sub.2 Me H CH.sub.2 OMe
OCOOPr-i SO.sub.2 Me H CH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me H
CH.sub.2 OMe OCONHMe SO.sub.2 Me H CH.sub.2 OMe OCONMe.sub.2
SO.sub.2 Me H CH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me H CH.sub.2
OMe Y20 SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me
H CH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H
CH.sub.2 OMe SCH.sub.2 CCH SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2
CF.sub.3 SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me
H CH.sub.2 OMe Y21 SO.sub.2 Me H CH.sub.2 OMe SPh SO.sub.2 Me H
CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe Y22 SO.sub.2 Me H
CH.sub.2 OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe S(O)CH.sub.2
CCH SO.sub.2 Me H CH.sub.2 OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me
H CH.sub.2 OMe Y23 SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2
CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2 CHCMe.sub.2
SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H
CH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H CH.sub.2 OMe
SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H CH.sub.2 OMe Y24
SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me H CH.sub.2 OMe
SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe SO.sub.2
CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2
Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2
Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2
Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2
OMe SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2
CH.sub.2 OMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl H CH.sub.2
OMe OCH.sub.2 CH.sub.2 OPr-i Cl H CH.sub.2 OMe OCHMeCH.sub.2 OMe Cl
H CH.sub.2 OMe OCH.sub.2 COOMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2
SMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H CH.sub.2
OMe SCH.sub.2 CH.sub.2 OMe Cl H CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2
Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2
OMe Cl CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2
CH.sub.2 OEt Cl CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh
______________________________________
TABLE 5 ______________________________________ ##STR36## X Y Z Q
______________________________________ Me Y1 SO.sub.2 Me H Me Y2
SO.sub.2 Me H Me Y3 SO.sub.2 Me H Me Y4 SO.sub.2 Me H Me Y5
SO.sub.2 Me H Me Y6 SO.sub.2 Me H Me Y7 SO.sub.2 Me H Me OCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Me OCHMeCH CH.sub.2 SO.sub.2 Me H Me
OCMe.sub.2 CH CH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CMe CH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CHCHMe SO.sub.2 Me H Me OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CH CH.sub.2
SO.sub.2 Me H Me OCH.sub.2 C CH SO.sub.2 Me H Me OCHMeC CH SO.sub.2
Me H Me OCHMe.sub.2 CCH SO.sub.2 Me H Me OCH.sub.2 CCMe SO.sub.2 Me
H Me OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Me OCH.sub.2 CHF.sub.2
SO.sub.2 Me H Me OCH.sub.2 CF.sub.3 SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Me OCH.sub.2 CCl.sub.3 SO.sub.2 Me H Me
OCHMeCH.sub.2 Cl SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H Me Y8 SO.sub.2
Me H Me OCH.sub.2 CCl CH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CCl CHCl
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me H Me OPh
SO.sub.2 Me H Me OPhMe-2 SO.sub.2 Me H Me OPhCl-4 SO.sub.2 Me H Me
OPhNO.sub.2 -4 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
H Me OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
OPr-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-i
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H Me OCH.sub.2 CH.sub.2Y4
SO.sub.2 Me H Me OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CHMeOMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 OH SO.sub.2 Me H Me OCH.sub.2 Ph SO.sub.2 Me H Me OCHMePh
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Me OCH.sub.2
Ph-2-Cl SO.sub.2 Me H Me OCH.sub.2 Ph-3-Me SO.sub.2 Me H Me
OCH.sub. 2 Ph-4-OMe SO.sub.2 Me H Me OCH.sub.2 Ph-4-NO.sub.2
SO.sub.2 Me H Me Y9 SO.sub.2 Me H Me Y10 SO.sub.2 Me H Me Y11
SO.sub.2 Me H Me Y12 SO.sub.2 Me H Me Y13 SO.sub.2 Me H Me Y14
SO.sub.2 Me H Me Y15 SO.sub.2 Me H Me Y16 SO.sub.2 Me H Me Y17
SO.sub.2 Me H Me Y18 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 NHPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NMe.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Me Y19
SO.sub.2 Me H Me OCH.sub.2 COOMe SO.sub.2 Me H Me OCH.sub.2 COOEt
SO.sub.2 Me H Me OCH.sub.2 COOPr-i SO.sub.2 Me H Me OCH.sub.2
COOBu-i SO.sub.2 Me H Me OCH.sub.2 COOBu-t SO.sub.2 Me H Me
OCH.sub.2 COOY4 SO.sub.2 Me H Me OCHMeCOOMe SO.sub.2 Me H Me
OCHMeCOOEt SO.sub.2 Me H Me OCHMeCOOPr-i SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H Me OCH.sub.2 SMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 S(O)Me
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
S(O)Pr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me H Me OCOOMe SO.sub.2 Me H Me OCOOPr-i SO.sub.2 Me H Me
OCONH.sub.2 SO.sub.2 Me H Me OCONHMe SO.sub.2 Me H Me OCONMe.sub.2
SO.sub.2 Me H Me OP(O)(OMe).sub.2 SO.sub.2 Me H Me Y20 SO.sub.2 Me
H Me SCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H Me SCH.sub.2 C CH SO.sub.2 Me H Me SCH.sub.2 CF.sub.3
SO.sub.2 Me H
Me SCH.sub.2 CCl.sub.3 SO.sub.2 Me H Me Y21 SO.sub.2 Me H Me SPh
SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me SCH.sub.2
CH.sub.2 OEt SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H Me Y22 SO.sub.2 Me H Me S(O)CH.sub.2 CH CH.sub.2 SO.sub.2 Me H Me
S(O)CH.sub.2 CH CMe.sub.2 SO.sub.2 Me H Me S(O)CH.sub.2 CCH
SO.sub.2 Me H Me S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me Y23
SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2 C
CH SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me Y24 SO.sub.2 Me H Me
Y25 SO.sub.2 Me H Me SO.sub.2 Ph SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CH.sub.2 OMe SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OEt
SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 OEt SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 Ph Me OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2
Ph Me OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
Me OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2
OEt Cl H Me OCH.sub.2 CH.sub.2 OPr-i Cl H Me OCHMeCH.sub.2 OMe Cl H
Me OCH.sub.2 COOMe Cl H Me OCH.sub.2 CH.sub.2 SMe Cl H Me OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Me SCH.sub.2 CH.sub.2 OMe Cl H Me
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 Ph Me SCH.sub.2 SH.sub.2 OMe Cl CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh Me
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh Me SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2
COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl Y1
SO.sub.2 Me H Cl Y2 SO.sub.2 Me H Cl Y3 SO.sub.2 Me H Cl Y4
SO.sub.2 Me H Cl Y5 SO.sub.2 Me H Cl Y6 SO.sub.2 Me H Cl Y7
SO.sub.2 Me H Cl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl OCHMeCH
CH.sub.2 SO.sub.2 Me H Cl OCMe.sub.2 CH CH.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CMe CH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CHCHMe SO.sub.2
Me H Cl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
CH CH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 C CH SO.sub.2 Me H Cl
OCHMeCCH SO.sub.2 Me H Cl OCHMe.sub.2 CCH SO.sub.2 Me H Cl
OCH.sub.2 CCMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 F SO.sub.2 Me H
Cl OCH.sub.2 CHF.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CF.sub.3 SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CCl.sub.3
SO.sub.2 Me H Cl OCHMeCH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 Br
SO.sub.2 Me H Cl Y8 SO.sub.2 Me H Cl OCH.sub.2 CCl CH.sub.2
SO.sub.2 Me H Cl OCH.sub.2 CCl CHCl SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 NO.sub.2 SO.sub.2 Me H Cl OPh SO.sub.2 Me H Cl OPhMe-2
SO.sub.2 Me
H Cl OPhCl-4 SO.sub.2 Me H Cl OPhNO.sub.2 -4 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-n
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-t
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me H Cl
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CHMeOMe SO.sub.2 Me H
Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OH SO.sub.2
Me H Cl OCH.sub.2 Ph SO.sub.2 Me H Cl OCHMePh SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Cl OCH.sub.2 Ph-2-Cl SO.sub.2
Me H Cl OCH.sub.2 Ph-3-Me SO.sub.2 Me H Cl OCH.sub.2 Ph-4-OMe
SO.sub.2 Me H Cl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me H Cl Y9
SO.sub.2 Me H Cl Y10 SO.sub.2 Me H Cl Y11 SO.sub.2 Me H Cl Y12
SO.sub.2 Me H Cl Y13 SO.sub.2 Me H Cl Y14 SO.sub.2 Me H Cl Y15
SO.sub.2 Me H Cl Y16 SO.sub.2 Me H Cl Y17 SO.sub.2 Me H Cl Y18
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NHPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Cl Y19 SO.sub.2 Me H Cl
OCH.sub.2 COOMe SO.sub.2 Me H Cl OCH.sub.2 COOEt SO.sub.2 Me H Cl
OCH.sub.2 COOPr-i SO.sub.2 Me H Cl OCH.sub.2 COOBu-i SO.sub.2 Me H
Cl OCH.sub.2 COOBu-t SO.sub.2 Me H Cl OCH.sub.2 COOY4 SO.sub.2 Me H
Cl OCHMeCOOMe SO.sub.2 Me H Cl OCHMeCOOEt SO.sub.2 Me H Cl
OCHMeCOOPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me H
Cl OCH.sub.2 SMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 CO.sub.2 Pr-i SO.sub.2 Me H Cl OCOOMe SO.sub.2
Me H Cl OCOOPr-i SO.sub.2 Me H Cl OCONH.sub.2 SO.sub.2 Me H Cl
OCONHMe SO.sub.2 Me H Cl OCONMe.sub.2 SO.sub.2 Me H Cl
OP(O)(OMe).sub.2 SO.sub.2 Me H Cl Y20 SO.sub.2 Me H Cl SCH.sub.2
CHCH.sub.2 SO.sub. 2 Me H Cl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl
SCH.sub.2 C CH SO.sub.2 Me H Cl SCH.sub.2 CF.sub.3 SO.sub.2 Me H Cl
SCH.sub.2 CCl.sub.3 SO.sub.2 Me H Cl Y21 SO.sub.2 Me H Cl SPh
SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl SCH.sub.2
CH.sub.2 OEt SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H Cl Y22 SO.sub.2 Me H Cl S(O)CH.sub.2 CH CH.sub.2 SO.sub.2 Me H Cl
S(O)CH.sub.2 CH CMe.sub.2 SO.sub.2 Me H Cl S(O)CH.sub.2 CCH
SO.sub.2 Me H Cl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl Y23
SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 C
CH SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl Y24 SO.sub.2 Me H Cl
Y25 SO.sub.2 Me H Cl SO.sub.2 Ph SO.sub.2 Me H Cl SO.sub.2 CH.sub.2
CH.sub.2 OMe SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 OEt
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SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe SO.sub.2
CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCHMeCH.sub.2 OMe SO.sub.2
Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2
Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2
Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Cl CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2
OMe SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub. 2 OPr-i SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2
CH.sub.2 OMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl H CH.sub.2
OMe OCH.sub.2 CH.sub.2 OPr-i Cl H CH.sub.2 OMe OCHMeCH.sub.2 OMe Cl
H CH.sub.2 OMe OCH.sub.2 COOMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2
SMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H CH.sub.2
OMe SCH.sub.2 CH.sub.2 OMe Cl H CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2
Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2
OMe Cl CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2
CH.sub.2 OEt Cl CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh
______________________________________
TABLE 6 ______________________________________ ##STR37## X Y Z Q
______________________________________ Me Y1 SO.sub.2 Me H Me Y2
SO.sub.2 Me H Me Y3 SO.sub.2 Me H Me Y4 SO.sub.2 Me H Me Y5
SO.sub.2 Me H Me Y6 SO.sub.2 Me H Me Y7 SO.sub.2 Me H Me OCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Me OCHMeCHCH.sub.2 SO.sub.2 Me H Me
OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CMeCH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CHCHMe SO.sub.2 Me H Me OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2
Me H Me OCH.sub.2 CCH SO.sub.2 Me H Me OCHMeC CH SO.sub.2 Me H Me
OCMe.sub.2 CCH SO.sub.2 Me H Me OCH.sub.2 CCMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Me OCH.sub.2 CHF.sub.2 SO.sub.2
Me H Me OCH.sub.2 CF.sub.3 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H Me OCH.sub.2 CCl.sub.3 SO.sub.2 Me H Me OCHMeCH.sub.2
Cl SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H Me Y8 SO.sub.2 Me H Me
OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CClCHCl SO.sub.2
Me H Me OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me H Me OPh SO.sub.2
Me H Me OPhMe-2 SO.sub.2 Me H Me OPhCl-4 SO.sub.2 Me H Me
OPhNO.sub.2 -4 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
H Me OCH.sub.2 CH.sub. 2 OEt SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
OPr-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-i
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H Me OCH.sub.2 CH.sub.2Y4
SO.sub.2 Me H Me OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CHMeOMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 OH SO.sub.2 Me H Me OCH.sub.2 Ph SO.sub.2 Me H Me OCHMePh
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Me OCH.sub.2
Ph-2-Cl SO.sub.2 Me H Me OCH.sub.2 Ph-3-Me SO.sub.2 Me H Me
OCH.sub.2 Ph-4-OMe SO.sub.2 Me H Me OCH.sub.2 Ph-4-NO.sub.2
SO.sub.2 Me H Me Y9 SO.sub.2 Me H Me Y10 SO.sub.2 Me H Me Y11
SO.sub.2 Me H Me Y12 SO.sub.2 Me H Me Y13 SO.sub.2 Me H Me Y14
SO.sub.2 Me H Me Y15 SO.sub.2 Me H Me Y16 SO.sub.2 Me H Me Y17
SO.sub.2 Me H Me Y18 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 NHPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NMe.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Me Y19
SO.sub.2 Me H Me OCH.sub.2 COOMe SO.sub.2 Me H Me OCH.sub.2 COOEt
SO.sub.2 Me H Me OCH.sub.2 COOPr-i SO.sub.2 Me H Me OCH.sub.2
COOBu-i SO.sub.2 Me H Me OCH.sub.2 COOBu-t SO.sub.2 Me H Me
OCH.sub.2 COOY4 SO.sub.2 Me H Me OCHMeCOOMe SO.sub.2 Me H Me
OCHMeCOOEt SO.sub.2 Me H Me OCHMeCOOPr-i SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H Me OCH.sub.2 SMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 S(O)Me
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
S(O)Pr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me H Me OCOOMe SO.sub.2 Me H Me OCOOPr-i SO.sub.2 Me H Me
OCONH.sub.2 SO.sub.2 Me H Me OCONHMe SO.sub.2 Me H Me OCONMe.sub.2
SO.sub.2 Me H Me OP(O)(OMe).sub.2 SO.sub.2 Me H Me Y20 SO.sub.2 Me
H Me SCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H Me SCH.sub.2 CCH SO.sub.2 Me H Me SCH.sub.2 CF.sub.3
SO.sub.2 Me H Me SCH.sub.2 CCl.sub.3
SO.sub.2 Me H Me Y21 SO.sub.2 Me H Me SPh SO.sub.2 Me H Me
SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me Y22
SO.sub.2 Me H Me S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Me S(O)CH.sub.2 CCH SO.sub.2
Me H Me S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me Y23 SO.sub.2 Me H
Me SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Me Y24 SO.sub.2 Me H Me Y25 SO.sub.2 Me H
Me SO.sub.2 Ph SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph Me OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
Me OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2
OEt Cl H Me OCH.sub.2 CH.sub.2 OPr-i Cl H Me OCHMeCH.sub.2 OMe Cl H
Me OCH.sub.2 COOMe Cl H Me OCH.sub.2 CH.sub.2 SMe Cl H Me OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Me SCH.sub.2 CH.sub.2 OMe Cl H Me
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Me OCH.sub. 2 CH.sub.2 SMe Cl CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh Me
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh Me SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2
COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl Y1
SO.sub.2 Me H Cl Y2 SO.sub.2 Me H Cl Y3 SO.sub.2 Me H Cl Y4
SO.sub.2 Me H Cl Y5 SO.sub.2 Me H Cl Y6 SO.sub.2 Me H Cl Y7
SO.sub.2 Me H Cl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
OCHMeCHCH.sub.2 SO.sub.2 Me H Cl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me
H Cl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CH CHMe
SO.sub.2 Me H Cl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CCH SO.sub.2 Me H Cl
OCHMeCCH SO.sub.2 Me H Cl OCMe.sub.2 CCH SO.sub.2 Me H Cl OCH.sub.2
CCMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Cl
OCH.sub.2 CHF.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CF.sub.3 SO.sub.2 Me
H Cl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CCl.sub.3
SO.sub.2 Me H Cl OCHMeCH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 Br
SO.sub.2 Me H Cl Y8 SO.sub.2 Me H Cl OCH.sub.2 CClCH.sub.2 SO.sub.2
Me H Cl OCH.sub.2 CClCHCl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
NO.sub.2 SO.sub.2 Me H Cl OPh SO.sub.2 Me H Cl OPhMe-2 SO.sub.2 Me
H
Cl OPhCl-4 SO.sub.2 Me H Cl OPhNO.sub.2 -4 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-n
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-t
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me H Cl
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CHMeOMe SO.sub.2 Me H
Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OH SO.sub.2
Me H Cl OCH.sub.2 Ph SO.sub.2 Me H Cl OCHMePh SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Cl OCH.sub.2 Ph-2-Cl SO.sub.2
Me H Cl OCH.sub.2 Ph-3-Me SO.sub.2 Me H Cl OCH.sub.2 Ph-4-OMe
SO.sub.2 Me H Cl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me H Cl Y9
SO.sub.2 Me H Cl Y10 SO.sub.2 Me H Cl Y11 SO.sub.2 Me H Cl Y12
SO.sub.2 Me H Cl Y13 SO.sub.2 Me H Cl Y14 SO.sub.2 Me H Cl Y15
SO.sub.2 Me H Cl Y16 SO.sub.2 Me H Cl Y17 SO.sub.2 Me H Cl Y18
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NHPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Cl Y19 SO.sub.2 Me H Cl
OCH.sub.2 COOMe SO.sub.2 Me H Cl OCH.sub.2 COOEt SO.sub.2 Me H Cl
OCH.sub.2 COOPr-i SO.sub.2 Me H Cl OCH.sub.2 COOBu-i SO.sub.2 Me H
Cl OCH.sub.2 COOBu-t SO.sub.2 Me H Cl OCH.sub.2 COOY4 SO.sub.2 Me H
Cl OCHMeCOOMe SO.sub.2 Me H Cl OCHMeCOOEt SO.sub.2 Me H Cl
OCHMeCOOPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me H
Cl OCH.sub.2 SMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H Cl OCOOMe SO.sub.2
Me H Cl OCOOPr-i SO.sub.2 Me H Cl OCONH.sub.2 SO.sub.2 Me H Cl
OCONHMe SO.sub.2 Me H Cl OCONMe.sub.2 SO.sub.2 Me H Cl
OP(O)(OMe).sub.2 SO.sub.2 Me H Cl Y20 SO.sub.2 Me H Cl SCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Cl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl
SCH.sub.2 C CH SO.sub.2 Me H Cl SCH.sub.2 CF.sub.3 SO.sub.2 Me H Cl
SCH.sub.2 CCl.sub.3 SO.sub.2 Me H Cl Y21 SO.sub.2 Me H Cl SPh
SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl SCH.sub.2
CH.sub.2 OEt SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H Cl Y22 SO.sub.2 Me H Cl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl S(O)CH.sub.2 CCH SO.sub.2
Me H Cl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl Y23 SO.sub.2 Me H
Cl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Cl Y24 SO.sub.2 Me H Cl Y25 SO.sub.2 Me H
Cl SO.sub.2 Ph SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph Cl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me
CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 Ph
Cl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 Ph Cl
SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl SCH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub. 2 Ph Cl SO.sub.2 CH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl SO.sub.2 CH.sub.2 CH.sub.2
OPr-i SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh
Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2
CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i
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OCH.sub.2 CH.sub.2 OPr-i Cl H Cl OCHMeCH.sub.2 OMe Cl H Cl
OCH.sub.2 COOMe Cl H Cl OCH.sub.2 CH.sub.2 SMe Cl H Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Cl SCH.sub.2 CH.sub.2 OMe Cl H Cl
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CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
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SO.sub.2 Me H
OMe Y5 SO.sub.2 Me H OMe Y6 SO.sub.2 Me H OMe Y7 SO.sub.2 Me H OMe
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H OMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CMeCH.sub.2
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Me H OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me H OMe OCH.sub.2 CHF.sub.2
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CH.sub.2 Cl SO.sub.2 Me H OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe
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SO.sub.2 Me H OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2
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OMe OPh SO.sub.2 Me H OMe OPhMe-2 SO.sub.2 Me H OMe OPhCl-4
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OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
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Me H OMe OCHMePh SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 Ph SO.sub.2
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Me H OMe Y11 SO.sub.2 Me H OMe Y12 SO.sub.2 Me H OMe Y13 SO.sub.2
Me H OMe Y14 SO.sub.2 Me H OMe Y15 SO.sub.2 Me H OMe Y16 SO.sub.2
Me H OMe Y17 SO.sub.2 Me H OMe Y18 SO.sub.2 Me H OMe OCH.sub.2
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OMe OCHMeCOOMe SO.sub.2 Me H OMe OCHMeCOOEt SO.sub.2 Me H OMe
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OMe OCH.sub.2 SMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2
Me H OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H OMe OCOOMe SO.sub.2
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CHCH.sub.2 SO.sub.2 Me H OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H
OMe SCH.sub.2 CCH SO.sub.2 Me H OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me
H OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe Y21 SO.sub.2 Me H OMe
SPh SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H OMe
SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2
OPr-i
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SO.sub.2 Me H OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H OMe
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CHCH.sub.2 SO.sub.2 Me H OMe SO.sub. 2 CH.sub.2 CHCMe.sub.2
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CH.sub.2 CF.sub.3 SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl
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SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H OMe OCH.sub.2
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CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2
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CH.sub.2 Ph OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe
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CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OMe
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CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
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CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe SO.sub.2 CH.sub.2 CH.sub. 2 OMe SO.sub.2 Me
CH.sub.2 COPh OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 OMe Cl H OMe OCH.sub.2
CH.sub.2 OEt Cl H OMe OCH.sub.2 CH.sub.2 OPr-i Cl H OMe
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CH.sub.2 SMe Cl H OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H OMe
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OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2
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CH.sub.2 OMe Y4 SO.sub.2 Me H CH.sub.2 OMe Y5 SO.sub.2 Me H
CH.sub.2 OMe Y6 SO.sub.2 Me H CH.sub.2 OMe Y7 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
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CH.sub.2 OMe OCHMeCCH SO.sub.2 Me H CH.sub. 2 OMe OCMe.sub.2 CCH
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me H CH.sub.2
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CHF.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me
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CH.sub.2 OMe OPhMe-2 SO.sub.2 Me H CH.sub.2 OMe OPhCl-4 SO.sub.2 Me
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SO.sub.2 Me H CH.sub.2 OMe Y12 SO.sub.2 Me H CH.sub.2 OMe Y13
SO.sub.2 Me H CH.sub.2 OMe Y14 SO.sub.2 Me H CH.sub.2 OMe Y15
SO.sub.2 Me H CH.sub.2 OMe Y16 SO.sub.2 Me H CH.sub.2 OMe Y17
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CH.sub.2 OMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H CH.sub.2
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CH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
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CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CHCMe.sub.2
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2 OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
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CH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H CH.sub.2 OMe
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CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2
COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2
COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2
Me CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OPr-i Cl H CH.sub.2 OMe OCHMeCH.sub.2 OMe Cl H CH.sub.2
OMe OCH.sub.2 COOMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OMe Cl H CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2
OMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2
OMe Cl CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2
CH.sub.2 OEt Cl CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh
______________________________________
TABLE 7 ______________________________________ ##STR38## X Y Z Q
______________________________________ Me Y1 SO.sub.2 Me H Me Y2
SO.sub.2 Me H Me Y3 SO.sub.2 Me H Me Y4 SO.sub.2 Me H Me Y5
SO.sub.2 Me H Me Y6 SO.sub.2 Me H Me Y7 SO.sub.2 Me H Me OCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Me OCHMeCHCH.sub.2 SO.sub.2 Me H Me
OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CMeCH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CHCHMe SO.sub.2 Me H Me OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2
Me H Me OCH.sub.2 CCH SO.sub.2 Me H Me OCHMeC CH SO.sub.2 Me H Me
OCMe.sub.2 CCH SO.sub.2 Me H Me OCH.sub.2 CCMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Me OCH.sub.2 CHF.sub.2 SO.sub.2
Me H Me OCH.sub.2 CF.sub.3 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H Me OCH.sub.2 CCl.sub.3 SO.sub.2 Me H Me OCHMeCH.sub.2
Cl SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H Me Y8 SO.sub.2 Me H Me
OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CClCHCl SO.sub.2
Me H Me OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me H Me OPh SO.sub.2
Me H Me OPhMe-2 SO.sub.2 Me H Me OPhCl-4 SO.sub.2 Me H Me
OPhNO.sub.2 -4 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
H Me OCH.sub.2 CH.sub.2 OEt SO.sub. 2 Me H Me OCH.sub.2 CH.sub.2
OPr-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-i
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 -Y4
SO.sub.2 Me H Me OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CHMeOMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 OH SO.sub.2 Me H Me OCH.sub.2 Ph SO.sub.2 Me H Me OCHMePh
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Me OCH.sub.2
Ph-2-Cl SO.sub.2 Me H Me OCH.sub.2 Ph-3-Me SO.sub.2 Me H Me
OCH.sub.2 Ph-4-OMe SO.sub.2 Me H Me OCH.sub.2 Ph-4-NO.sub.2
SO.sub.2 Me H Me Y9 SO.sub.2 Me H Me Y10 SO.sub.2 Me H Me Y11
SO.sub.2 Me H Me Y12 SO.sub.2 Me H Me Y13 SO.sub.2 Me H Me Y14
SO.sub.2 Me H Me Y15 SO.sub.2 Me H Me Y16 SO.sub.2 Me H Me Y17
SO.sub.2 Me H Me Y18 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 NHPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NMe.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Me Y19
SO.sub.2 Me H Me OCH.sub.2 COOMe SO.sub.2 Me H Me OCH.sub.2 COOEt
SO.sub.2 Me H Me OCH.sub.2 COOPr-i SO.sub.2 Me H Me OCH.sub.2
COOBu-i SO.sub.2 Me H Me OCH.sub.2 COOBu-t SO.sub.2 Me H Me
OCH.sub.2 COO-Y4 SO.sub.2 Me H Me OCHMeCOOMe SO.sub.2 Me H Me
OCHMeCOOEt SO.sub.2 Me H Me OCHMeCOOPr-i SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H Me OCH.sub.2 SMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 S(O)Me
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
S(O)Pr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me H Me OCOOMe SO.sub.2 Me H Me OCOOPr-i SO.sub.2 Me H Me
OCONHG.sub.2 SO.sub.2 Me H Me OCONHMe SO.sub.2 Me H Me OCONMe.sub.2
SO.sub.2 Me H Me OP(O)(OMe).sub.2 SO.sub.2 Me H Me Y20 SO.sub.2 Me
H Me SCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H Me SCH.sub.2 CCH SO.sub.2 Me H Me SCH.sub.2 CF.sub.3
SO.sub.2 Me H Me SCH.sub.2 CCl.sub.3
SO.sub.2 Me H Me Y21 SO.sub.2 Me H Me SPh SO.sub.2 Me H Me
SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me SCH.sub.2 CH.sub. 2 OEt
SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me Y22
SO.sub.2 Me H Me S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Me S(O)CH.sub.2 CCH SO.sub.2
Me H Me S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me Y23 SO.sub.2 Me H
Me SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Me Y24 SO.sub.2 Me H Me Y25 SO.sub.2 Me H
Me SO.sub.2 Ph SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph Me OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
Me OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2
OEt Cl H Me OCH.sub.2 CH.sub.2 OPr-i Cl H Me OCHMeCH.sub.2 OMe Cl H
Me OCH.sub.2 COOMe Cl H Me OCH.sub.2 CH.sub.2 SMe Cl H Me OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Me SCH.sub.2 CH.sub.2 OMe Cl H Me
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh Me
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh Me SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2
COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl Y1
SO.sub.2 Me H Cl Y2 SO.sub.2 Me H Cl Y3 SO.sub.2 Me H Cl Y4
SO.sub.2 Me H Cl Y5 SO.sub.2 Me H Cl Y6 SO.sub.2 Me H Cl Y7
SO.sub.2 Me H Cl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
OCHMeCHCH.sub.2 SO.sub.2 Me H Cl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me
H Cl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CHCHMe
SO.sub.2 Me H Cl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CCH SO.sub.2 Me H Cl
OCHMeCCH SO.sub.2 Me H Cl OCMe.sub.2 CCH SO.sub.2 Me H Cl OCH.sub.2
CCMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Cl
OCH.sub.2 CHF.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CF.sub.3 SO.sub.2 Me
H Cl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CCl.sub.3
SO.sub.2 Me H Cl OCHMeCH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 Br
SO.sub.2 Me H Cl Y8 SO.sub.2 Me H Cl OCH.sub.2 CClCH.sub.2 SO.sub.2
Me H Cl OCH.sub.2 CClCHCl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
NO.sub. 2 SO.sub.2 Me H Cl OPh SO.sub.2 Me H Cl OPh-Me-2 SO.sub.2
Me H
Cl OPh-Cl-4 SO.sub.2 Me H Cl OPh-NO.sub.2 -4 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-n
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-t
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2-Y4 SO.sub.2 Me H Cl
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CHMeOMe SO.sub.2 Me H
Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OH SO.sub.2
Me H Cl OCH.sub.2 Ph SO.sub.2 Me H Cl OCHMePh SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Cl OCH.sub.2 Ph-2-Cl SO.sub.2
Me H Cl OCH.sub.2 Ph-3-Me SO.sub.2 Me H Cl OCH.sub.2 Ph-4-OMe
SO.sub.2 Me H Cl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me H Cl Y9
SO.sub.2 Me H Cl Y10 SO.sub.2 Me H Cl Y11 SO.sub.2 Me H Cl Y12
SO.sub.2 Me H Cl Y13 SO.sub.2 Me H Cl Y14 SO.sub.2 Me H Cl Y15
SO.sub.2 Me H Cl Y16 SO.sub.2 Me H Cl Y17 SO.sub.2 Me H Cl Y18
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NHPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Cl Y19 SO.sub.2 Me H Cl
OCH.sub.2 COOMe SO.sub.2 Me H Cl OCH.sub.2 COOEt SO.sub.2 Me H Cl
OCH.sub.2 COOPr-i SO.sub.2 Me H Cl OCH.sub.2 COOBu-i SO.sub.2 Me H
Cl OCH.sub.2 COOBu-t SO.sub.2 Me H Cl OCH.sub.2 COO-Y4 SO.sub.2 Me
H Cl OCHMeCOOMe SO.sub.2 Me H Cl OCHMeCOOEt SO.sub.2 Me H Cl
OCHMeCOOPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me H
Cl OCH.sub.2 SMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H Cl OCOOMe SO.sub.2
Me H Cl OCOOPr-i SO.sub.2 Me H Cl OCONH.sub.2 SO.sub.2 Me H Cl
OCONHMe SO.sub.2 Me H Cl OCONMe.sub.2 SO.sub.2 Me H Cl
OP(O)(OMe).sub.2 SO.sub.2 Me H Cl Y20 SO.sub.2 Me H Cl SCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Cl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl
SCH.sub.2 CCH SO.sub. 2 Me H Cl SCH.sub.2 CF.sub.3 SO.sub.2 Me H Cl
SCH.sub.2 CCl.sub.3 SO.sub.2 Me H Cl Y21 SO.sub.2 Me H Cl SPh
SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl SCH.sub.2
CH.sub.2 OEt SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H Cl Y22 SO.sub.2 Me H Cl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl S(O)CH.sub.2 CCH SO.sub.2
Me H Cl S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl Y23 SO.sub.2 Me H
Cl SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Cl Y24 SO.sub.2 Me H Cl Y25 SO.sub.2 Me H
Cl SO.sub.2 Ph SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 cH.sub.2 OEt SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph Cl OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.3 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me
CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me CH.sub.2 Ph
Cl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 Ph Cl
SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl SCH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Cl SO.sub.2 CH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl SO.sub.2 CH.sub.2 CH.sub.2
OPr-i SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh
Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2
CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i
SO.sub.2 Me CH.sub.2 COPh Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Cl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh
Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh Cl
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh Cl
OCH.sub.2 CH.sub.2 OMe Cl H Cl OCH.sub.2 CH.sub.2 OEt Cl H Cl
OCH.sub.2 CH.sub.2 OPr-i Cl H Cl OCHMeCH.sub.2 OMe Cl H Cl
OCH.sub.2 COOMe Cl H Cl OCH.sub.2 CH.sub. 2 SMe Cl H Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Cl SCH.sub.2 CH.sub.2 OMe Cl H Cl
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H Cl OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 Ph Cl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Cl SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh Cl
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh Cl SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh Cl SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2
COPh Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh OMe Y1
SO.sub.2 Me H OMe Y2 SO.sub.2 Me H OMe Y3 SO.sub.2 Me H OMe Y4
SO.sub.2 Me H
OMe Y5 SO.sub.2 Me H OMe Y6 SO.sub.2 Me H OMe Y7 SO.sub.2 Me H OMe
OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe OCHMdCHCH.sub.2 SO.sub.2 Me
H OMe OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CMeCH.sub.2
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Me H OMe OCMe.sub.2 CCH SO.sub.2 Me H OMe OCH.sub.2 CCMe SO.sub.2
Me H OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me H OMe OCH.sub.2 CHF.sub.2
SO.sub.2 Me H OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 Cl SO.sub.2 Me H OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe
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SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H OMe Y8
SO.sub.2 Me H OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2
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OMe OPh SO.sub.2 Me H OMe OPhMe-2 SO.sub.2 Me H OMe OPhCl-4
SO.sub.2 Me H OMe OPhNO.sub.2 -4 SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H
OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
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SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H OMe
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Me H OMe OCHMePh SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 Ph SO.sub.2
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Ph-4-NO.sub.2 SO.sub.2 Me H OMe Y9 SO.sub.2 Me H OMe Y10 SO.sub.2
Me H OMe Y11 SO.sub.2 Me H OMe Y12 SO.sub.2 Me H OMe Y13 SO.sub.2
Me H OMe Y14 SO.sub.2 Me H OMe Y15 SO.sub.2 Me H OMe Y16 SO.sub.2
Me H OMe Y17 SO.sub.2 Me H OMe Y18 SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 NH.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NHMe
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OMe OCHMeCOOMe SO.sub.2 Me H OMe OCHMeCOOEt SO.sub.2 Me H OMe
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OMe OCH.sub.2 SMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2
Me H OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H OMe OCOOMe SO.sub.2
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OCONHMe SO.sub.2 Me H OMe OCONMe.sub. 2 SO.sub.2 Me H OMe
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CHCH.sub.2 SO.sub.2 Me H OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H
OMe SCH.sub.2 CCH SO.sub.2 Me H OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me
H OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe Y21 SO.sub.2 Me H OMe
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SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2
OPr-i
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CF.sub.3 SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2
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CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph
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OMe SCH.sub.2 CH.sub.2 OMe Cl H OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe
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CH.sub.2 OMe Y4 SO.sub.2 Me H CH.sub.2 OMe Y5 SO.sub.2 Me H
CH.sub.2 OMe Y6 SO.sub.2 Me H CH.sub.2 OMe Y7 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
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CH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
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CH.sub.2 OMe OCHMeCCH SO.sub.2 Me H CH.sub.2 OMe OCMe.sub.2 C CH
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CCMe SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CHF.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me
H CH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H CH.sub.2 OMe
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CH.sub.2 OMe OCH.sub.2 CClCHCl SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 NO.sub.2 SO.sub.2 Me H CH.sub.2 OMe OPh SO.sub.2 Me H
CH.sub.2 OMe OPhMe-2 SO.sub.2 Me H CH.sub.2 OMe OPhCl-4 SO.sub.2 Me
H CH.sub.2 OMe OPh N.sub.2 -4 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
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CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe
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CH.sub.2 OBu-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s
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CH.sub.2 OMe OCH.sub.2 CH.sub.2 -Y4 SO.sub.2 Me H CH.sub.2 OMe
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SO.sub.2 Me H CH.sub.2 OMe Y10 SO.sub.2 Me H CH.sub.2 OMe Y11
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SO.sub.2 Me H CH.sub.2 OMe Y14 SO.sub.2 Me H CH.sub.2 OMe Y15
SO.sub.2 Me H CH.sub.2 OMe Y16 SO.sub.2 Me H CH.sub.2 OMe Y17
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CH.sub.2 OMe OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H CH.sub.2
OMe Y19 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOMe SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
COOPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOBu-i SO.sub.2 Me H
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OMe OCHMeCOOEt SO.sub.2 Me H CH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me
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CH.sub.2 S(O)Pr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me H CH.sub.2 OMe OCOOMe SO.sub.2 Me H
CH.sub.2 OMe OCOOPr-i SO.sub.2 Me H CH.sub.2 OMe OCONH.sub.2
SO.sub.2 Me H CH.sub.2 OMe OCONHMe SO.sub.2 Me H CH.sub.2 OMe
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CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H CH.sub.2 OMe
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CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe
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CH.sub.2 OMe S(O)CH.sub.2 CH CH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
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OMe Cl CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2
CH.sub.2 OEt Cl CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh
______________________________________
TABLE 8 ______________________________________ ##STR39## X Y Z Q
______________________________________ Me Y1 SO.sub.2 Me H Me Y2
SO.sub.2 Me H Me Y3 SO.sub.2 Me H Me Y4 SO.sub.2 Me H Me Y5
SO.sub.2 Me H Me Y6 SO.sub.2 Me H Me Y7 SO.sub.2 Me H Me OCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Me OCHMeCHCH.sub.2 SO.sub.2 Me H Me
OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CMeCH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CHCHMe SO.sub.2 Me H Me OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2
Me H Me OCH.sub.2 CCH SO.sub.2 Me H Me OCHMeC CH SO.sub.2 Me H Me
OCMe.sub.2 CCH SO.sub.2 Me H Me OCH.sub.2 CCMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Me OCH.sub.2 CHF.sub.2 SO.sub.2
Me H Me OCH.sub.2 CF.sub.3 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H Me OCH.sub.2 CCl.sub.3 SO.sub.2 Me H Me OCHMeCH.sub.2
Cl SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H Me Y8 SO.sub.2 Me H Me
OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H Me OCH.sub.2 CClCHCl SO.sub.2
Me H Me OCH.sub.2 CH.sub.2 NO.sub.2 SO.sub.2 Me H Me OPh SO.sub.2
Me H Me OPhMe-2 SO.sub.2 Me H Me OPhCl-4 SO.sub.2 Me H Me
OPhNO.sub.2 -4 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
H Me OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
OPr-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-n SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-i
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Y4
SO.sub.2 Me H Me OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CHMeOMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 OH SO.sub.2 Me H Me OCH.sub.2 Ph SO.sub.2 Me H Me OCHMePh
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Me OCH.sub.2
Ph-2-Cl SO.sub.2 Me H Me OCH.sub.2 Ph-3-Me SO.sub.2 Me H Me
OCH.sub.2 Ph-4-OMe SO.sub.2 Me H Me OCH.sub.2 Ph-4-NO.sub.2
SO.sub.2 Me H Me Y9 SO.sub.2 Me H Me Y10 SO.sub.2 Me H Me Y11
SO.sub.2 Me H Me Y12 SO.sub.2 Me H Me Y13 SO.sub.2 Me H Me Y14
SO.sub.2 Me H Me Y15 SO.sub.2 Me H Me Y16 SO.sub.2 Me H Me Y17
SO.sub.2 Me H Me Y18 SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NH.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 NHPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NMe.sub.2
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Me Y19
SO.sub.2 Me H Me OCH.sub.2 COOMe SO.sub.2 Me H Me OCH.sub.2 COOEt
SO.sub.2 Me H Me OCH.sub.2 COOPr-i SO.sub.2 Me H Me OCH.sub.2
COOBu-i SO.sub.2 Me H Me OCH.sub.2 COOBu-t SO.sub.2 Me H Me
OCH.sub.2 COOY4 SO.sub.2 Me H Me OCHMeCOOMe SO.sub.2 Me H Me
OCHMeCOOEt SO.sub.2 Me H Me OCHMeCOOPr-i SO.sub.2 Me H Me OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H Me OCH.sub.2 SMe SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 S(O)Me
SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Me
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2
S(O)Pr-i SO.sub.2 Me H Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2
Me H Me OCOOMe SO.sub.2 Me H Me OCOOPr-i SO.sub.2 Me H Me
OCONH.sub.2 SO.sub.2 Me H Me OCONHMe SO.sub.2 Me H Me OCONMe.sub.2
SO.sub.2 Me H Me OP(O)(OMe).sub.2 SO.sub.2 Me H Me Y20 SO.sub.2 Me
H Me SCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H Me SCH.sub.2 CCH SO.sub.2 Me H Me SCH.sub.2 CF.sub.3
SO.sub.2 Me H Me SCH.sub.2 CCl.sub.3
SO.sub.2 Me H Me Y21 SO.sub.2 Me H Me SPh SO.sub.2 Me H Me
SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Me SCH.sub.2 CH.sub. 2 OEt
SO.sub.2 Me H Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me Y22
SO.sub.2 Me H Me S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Me S(O)CH.sub.2 CCH SO.sub.2
Me H Me S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Me Y23 SO.sub.2 Me H
Me SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CHCMe.sub.2 SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H Me SO.sub.2 CH.sub.2
CH.sub.2 Cl SO.sub.2 Me H Me Y24 SO.sub.2 Me H Me Y25 SO.sub.2 Me H
Me SO.sub.2 Ph SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H Me SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H Me
SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Me OCH.sub. 2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 Ph Me OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Me SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub. 2 SMe SO.sub.2 Me CH.sub.2 COPh
Me OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh Me OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2
OEt Cl H Me OCH.sub.2 CH.sub.2 OPr-i Cl H Me OCHMeCH.sub.2 OMe Cl H
Me OCH.sub.2 COOMe Cl H Me OCH.sub.2 CH.sub.2 SMe Cl H Me OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl H Me SCH.sub.2 CH.sub.2 OMe Cl H Me
SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph Me OCH.sub.2
CH.sub.2 SOMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl
CH.sub.2 Ph Me SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Me OCH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh Me OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh Me
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh Me SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh Me SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2
COPh Me SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl Y1
SO.sub.2 Me H Cl Y2 SO.sub.2 Me H Cl Y3 SO.sub.2 Me H Cl Y4
SO.sub.2 Me H Cl Y5 SO.sub.2 Me H Cl Y6 SO.sub.2 Me H Cl Y7
SO.sub.2 Me H Cl OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
OCHMeCHCH.sub.2 SO.sub.2 Me H Cl OCMe.sub.2 CHCH.sub.2 SO.sub.2 Me
H Cl OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CHCHMe
SO.sub.2 Me H Cl OCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CCH SO.sub.2 Me H Cl
OCHMeCCH SO.sub.2 Me H Cl OCMe.sub.2 CCH SO.sub.2 Me H Cl OCH.sub.2
CCMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 F SO.sub.2 Me H Cl
OCH.sub.2 CHF.sub.2 SO.sub.2 Me H Cl OCH.sub.2 CF.sub.3 SO.sub.2 Me
H Cl OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CCl.sub.3
SO.sub.2 Me H Cl OCHMeCH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 Br
SO.sub.2 Me H Cl Y8 SO.sub.2 Me H Cl OCH.sub.2 CClCH.sub.2 SO.sub.2
Me H Cl OCH.sub.2 CClCHCl SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
NO.sub.2 SO.sub.2 Me H Cl OPh SO.sub.2 Me H Cl OPhMe-2 SO.sub.2 Me
H
Cl OPhCl-4 SO.sub.2 Me H Cl OPhNO.sub.2 -4 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-n
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OBu-t
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me H Cl
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CHMeOMe SO.sub.2 Me H
Cl OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2
OCHMeCH.sub.2 OMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OH SO.sub.2
Me H Cl OCH.sub.2 Ph SO.sub.2 Me H Cl OCHMePh SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H Cl OCH.sub.2 Ph-2-Cl SO.sub.2
Me H Cl OCH.sub.2 Ph-3-Me SO.sub.2 Me H Cl OCH.sub.2 Ph-4-OMe
SO.sub.2 Me H Cl OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me H Cl Y9
SO.sub.2 Me H Cl Y10 SO.sub.2 Me H Cl Y11 SO.sub.2 Me H Cl Y12
SO.sub.2 Me H Cl Y13 SO.sub.2 Me H Cl Y14 SO.sub.2 Me H Cl Y15
SO.sub.2 Me H Cl Y16 SO.sub.2 Me H Cl Y17 SO.sub.2 Me H Cl Y18
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NHPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H Cl Y19 SO.sub.2 Me H Cl
OCH.sub.2 COOMe SO.sub.2 Me H Cl OCH.sub.2 COOEt SO.sub.2 Me H Cl
OCH.sub.2 COOPr-i SO.sub.2 Me H Cl OCH.sub.2 COOBu-i SO.sub.2 Me H
Cl OCH.sub.2 COOBu-t SO.sub.2 Me H Cl OCH.sub.2 COO-Y4 SO.sub.2 Me
H Cl OCHMeCOOMe SO.sub.2 Me H Cl OCHMeCOOEt SO.sub.2 Me H Cl
OCHMeCOOPr-i SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 CN SO.sub.2 Me H
Cl OCH.sub.2 SMe SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2
Me H Cl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H Cl OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me H Cl
OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H Cl OCOOMe SO.sub.2
Me H Cl OCOOPr-i SO.sub.2 Me H Cl OCONH.sub.2 SO.sub.2 Me H Cl
OCONHMe SO.sub.2 Me H Cl OCONMe.sub.2 SO.sub.2 Me H Cl
OP(O)(OMe).sub.2 SO.sub.2 Me H Cl Y20 SO.sub.2 Me H Cl SCH.sub.2
CHCH.sub.2 SO.sub.2 Me H Cl SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl
SCH.sub.2 C CH SO.sub.2 Me H Cl SCH.sub.2 CF.sub.3 SO.sub.2 Me H Cl
SCH.sub.2 CCl.sub.3 SO.sub.2 Me H Cl Y21 SO.sub.2 Me H Cl SPh
SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl SCH.sub.2
CH.sub.2 OEt SO.sub.2 Me H Cl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H Cl Y22 SO.sub.2 Me H Cl S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H Cl
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl S(O)CH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H Cl Y23 SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CHCH.sub.2
SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CCH SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CF.sub.3
SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H Cl Y24
SO.sub.2 Me H Cl Y25 SO.sub.2 Me H Cl SO.sub.2 Ph SO.sub.2 Me H Cl
SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H Cl SO.sub.2 CH.sub.2
CH.sub.2 OEt SO.sub.2 Me H Cl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me H Cl OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl
OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Cl OCHMeCH.sub.2 OMe
SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me
CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph Cl
OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2
S(O)Pr-i
SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i
SO.sub.2 Me CH.sub.2 Ph Cl SCH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 Ph Cl SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Cl
SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph Cl SO.sub.2
CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph Cl OCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me
CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh
Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh Cl
OCH.sub.2 CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2
CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh Cl SCH.sub.2
CH.sub.2 OMe SO.sub.2 Me CH.sub.2 COPh Cl SCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 COPh Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh Cl SO.sub.2 CH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 OMe Cl H Cl
OCH.sub.2 CH.sub.2 OEt Cl H Cl OCH.sub.2 CH.sub.2 OPr-i Cl H Cl
OCHMeCH.sub.2 OMe Cl H Cl OCH.sub.2 COOMe Cl H Cl OCH.sub.2
CH.sub.2 SMe Cl H Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H Cl
SCH.sub.2 CH.sub.2 OMe Cl H Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H
Cl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SMe
Cl CH.sub.2 Ph Cl OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 Ph Cl
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph Cl SCH.sub.2 CH.sub.2
OMe Cl CH.sub.2 Ph Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph
Cl OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2
SMe Cl CH.sub.2 COPh Cl OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2
COPh Cl SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh Cl SCH.sub.2
CH.sub.2 OEt Cl CH.sub.2 COPh Cl SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 COPh OMe Y1 SO.sub.2 Me H OMe Y2 SO.sub.2 Me H OMe Y3
SO.sub.2 Me H OMe Y4 SO.sub.2 Me H OMe Y5 SO.sub.2 Me H
OMe Y6 SO.sub.2 Me H OMe Y7 SO.sub.2 Me H OMe OCH.sub.2 CHCH.sub.2
SO.sub.2 Me H OMe OCHMeCHCH.sub.2 SO.sub. 2 Me H OMe OCMe.sub.2
CHCH.sub.2 SO.sub.2 Me H OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H
OMe OCH.sub.2 CHCHMe SO.sub.2 Me H OMe OCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe
OCH.sub.2 CCH SO.sub.2 Me H OMe OCHMeCCH SO.sub.2 Me H OMe
OCMe.sub.2 CCH SO.sub.2 Me H OMe OCH.sub.2 CCMe SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 F SO.sub.2 Me H OMe OCH.sub.2 CHF.sub.2 SO.sub.2
Me H OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H OMe OCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe
OCHMeCH.sub.2 Cl SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H OMe Y8
SO.sub. 2 Me H OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H OMe
OCH.sub.2 CClCHCl SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NO.sub.2
SO.sub.2 Me H OMe OPh SO.sub.2 Me H OMe OPhMe-2 SO.sub.2 Me H OMe
OPhCl-4 SO.sub.2 Me H OMe OPhNO.sub.2 -4 SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OEt
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-n
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-i SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OBu-t
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me H OMe
OCHMeCH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CHMeOMe SO.sub.2 Me H
OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
OCH.sub.2 CH.sub. 2 OPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2
OCHMeCH.sub.2 OMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 OH SO.sub.2
Me H OMe OCH.sub.2 Ph SO.sub.2 Me H OMe OCHMePh SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 Ph SO.sub.2 Me H OMe OCH.sub.2 Ph-2-Cl SO.sub.2
Me H OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me H OMe OCH.sub.2 Ph-4-OMe
SO.sub.2 Me H OMe OCH.sub.2 Ph-4-NO.sub.2 SO.sub.2 Me H OMe Y9
SO.sub.2 Me H OMe Y10 SO.sub.2 Me H OMe Y11 SO.sub.2 Me H OMe Y12
SO.sub.2 Me H OMe Y13 SO.sub.2 Me H OMe Y14 SO.sub.2 Me H OMe Y15
SO.sub.2 Me H OMe Y16 SO.sub.2 Me H OMe Y17 SO.sub.2 Me H OMe Y18
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NHPr-i
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 NMe.sub.2 SO.sub.2 Me H OMe
OCH.sub.2 CH.sub.2 NEt.sub.2 SO.sub.2 Me H OMe Y19 SO.sub.2 Me H
OMe OCH.sub.2 COOMe SO.sub.2 Me H OMe OCH.sub.2 COOEt SO.sub.2 Me H
OMe OCH.sub.2 COOPr-i SO.sub.2 Me H OMe OCH.sub.2 COOBu-i SO.sub.2
Me H OMe OCH.sub.2 COOBu-t SO.sub.2 Me H OMe OCH.sub.2 COOY4
SO.sub.2 Me H OMe OCHMeCOOMe SO.sub.2 Me H OMe OCHMeCOOEt SO.sub.2
Me H OMe OCHMeCOOPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 CN
SO.sub.2 Me H OMe OCH.sub.2 SMe SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 SMe SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2
Me H OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me SO.sub.2 Me H OMe OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 S(O)Pr-i
SO.sub.2 Me H OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me H
OMe OCOOMe SO.sub.2 Me H OMe OCOOPr-i SO.sub.2 Me H OMe OCONH.sub.2
SO.sub.2 Me H OMe OCONHMe SO.sub.2 Me H OMe OCONME.sub.2 SO.sub.2
Me H OMe OP(O)(OMe).sub.2 SO.sub.2 Me H OMe Y20 SO.sub.2 Me H OMe
SCH.sub. 2 CHCH.sub.2 SO.sub.2 Me H OMe SCH.sub.2 CHCMe.sub.2
SO.sub.2 Me H OMe SCH.sub.2 CCH SO.sub.2 Me H OMe SCH.sub.2
CF.sub.3 SO.sub.2 Me H OMe SCH.sub.2 CCl.sub.3 SO.sub.2 Me H OMe
Y21 SO.sub.2 Me H OMe SPh SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H OMe
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H
OMe Y22 SO.sub.2 Me H OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe
S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H OMe S(O)CH.sub.2 CCH
SO.sub.2 Me H OMe S(O)CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H OMe Y23
SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H OMe
SO.sub.2 CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H OMe SO.sub.2 CH.sub.2
CCH SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2 Me H OMe
SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H OMe Y24 SO.sub.2 Me H
OMe Y25 SO.sub.2 Me H OMe SO.sub.2 Ph SO.sub.2 Me H OMe SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CH.sub.2
OEt SO.sub.2 Me H OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
H OMe OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2
CH.sub.2 OEt SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 Ph OMe OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2
Ph OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2
CH.sub.2 S(O)Me SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2
SO.sub.2 Me SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 S(O)Pr-i SO.sub.2 Me
CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i SO.sub.2 Me
CH.sub.2 Ph OMe SCH.sub. 2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe
SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph OMe SO.sub.2
CH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph OMe SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me CH.sub.2 COPh
OMe OCH.sub.2 CH.sub.2 SOMe SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2
CH.sub.2 SPr-i SO.sub.2 Me CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2
SO.sub.2 Pr-i SO.sub.2 Me CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me
CH.sub.2 COPh OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me
CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2 OMe Cl H OMe OCH.sub. 2
CH.sub.2 OEt Cl H OMe OCH.sub.2 CH.sub.2 OPr-i Cl H OMe
OCHMeCH.sub.2 OMe Cl H OMe OCH.sub.2 COOMe Cl H OMe OCH.sub.2
CH.sub.2 SMe Cl H OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H OMe
SCH.sub.2 CH.sub.2 OMe Cl H OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl H
OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2
SMe Cl CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 Ph OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph OMe SCH.sub.2
CH.sub.2 OMe Cl CH.sub.2 Ph OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh OMe
OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh OMe OCH.sub.2 CH.sub.2
SO.sub.2 Me Cl CH.sub.2 COPh OMe SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2
COPh OMe SCH.sub.2 CH.sub.2 OEt Cl CH.sub.2 COPh OMe SO.sub.2
CH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe Y1 SO.sub.2 Me
H CH.sub.2 OMe Y2 SO.sub.2 Me H CH.sub.2 OMe Y3 SO.sub.2 Me H
CH.sub.2 OMe Y4 SO.sub.2 Me H CH.sub.2 OMe Y5 SO.sub.2 Me H
CH.sub.2 OMe Y6 SO.sub.2 Me H CH.sub.2 OMe Y7 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
OCHMeCHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCHMe.sub.2 CHCH.sub.2
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CMeCH.sub.2 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CHCHMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CCH SO.sub.2 Me H
CH.sub.2 OMe OCHMeCCH SO.sub.2 Me H CH.sub.2 OMe OCMe.sub.2 CCH
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CCMe SO.sub. 2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 F SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CHF.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CF.sub.3 SO.sub.2 Me
H CH.sub.2 OMe OCH.sub.2 CH.sub.2 Cl SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CCl.sub.3 SO.sub.2 Me H CH.sub.2 OMe OCHMeCH.sub.2 Cl
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2
Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 Br SO.sub.2 Me H CH.sub.2 OMe
Y8 SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CClCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CClCHCl SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
NO.sub.2 SO.sub.2 Me H CH.sub.2 OMe OPh SO.sub.2 Me H CH.sub.2 OMe
OPhMe-2 SO.sub.2 Me H CH.sub.2 OMe OPhCl-4 SO.sub.2 Me H CH.sub.2
OMe OPhNO.sub.2 -4 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
OMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-n SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OBu-n SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-i
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-s SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 OBu-t SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2Y4 SO.sub.2 Me H CH.sub.2 OMe OCHMeCH.sub.2 OMe
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CHMeOMe SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 OPh SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 CH.sub.2 OCHMeCH.sub.2 OMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OH SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph
SO.sub.2 Me H CH.sub.2 OMe OCHMePh SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub. 2 Ph SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph-2-Cl
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 Ph-3-Me SO.sub.2 Me H CH.sub.2
OMe OCH.sub.2 Ph-4-OMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
Ph-4-NO.sub.2 SO.sub.2 Me H CH.sub.2 OMe Y9 SO.sub.2 Me H CH.sub.2
OMe Y10 SO.sub.2 Me H CH.sub.2 OMe Y11 SO.sub.2 Me H CH.sub.2 OMe
Y12 SO.sub.2 Me H CH.sub.2 OMe Y13 SO.sub.2 Me H CH.sub.2 OMe Y14
SO.sub.2 Me H CH.sub.2 OMe Y15 SO.sub.2 Me H CH.sub.2 OMe Y16
SO.sub.2 Me H CH.sub.2 OMe Y17 SO.sub.2 Me H CH.sub.2 OMe Y18
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 NH.sub.2 SO.sub.2 Me
H CH.sub.2 OMe OCH.sub.2 CH.sub.2 NHMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 NHPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 NMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
NEt.sub.2 SO.sub.2 Me H CH.sub.2 OMe Y19 SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 COOMe SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOEt SO.sub.2
Me H CH.sub.2 OMe OCH.sub.2 COOPr-i SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 COOBu-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOBu-t
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 COOY4 SO.sub.2 Me H CH.sub.2
OMe OCHMeCOOMe SO.sub.2 Me H CH.sub.2 OMe OCHMeCOOEt SO.sub.2 Me H
CH.sub.2 OMe OCHMeCOOPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 CN SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 SMe SO.sub.2 Me H
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 S(O)Me SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2
SPr-i SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i
SO.sub.2 Me H CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Pr-i
SO.sub.2 Me H CH.sub.2 OMe OCOOMe SO.sub.2 Me H CH.sub.2 OMe
OCOOPr-i SO.sub.2 Me H CH.sub.2 OMe OCONH.sub.2 SO.sub.2 Me H
CH.sub.2 OMe OCONHME SO.sub.2 Me H CH.sub.2 OMe OCONMe.sub.2
SO.sub.2 Me H CH.sub.2 OMe OP(O)(OMe).sub.2 SO.sub.2 Me H CH.sub.2
OMe Y20 SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CHCH.sub.2 SO.sub.2 Me
H CH.sub.2 OMe SCH.sub.2 CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe
SCH.sub.2 CCH SO.sub.2 Me H
CH.sub.2 OMe SCH.sub.2 CF.sub.3 SO.sub.2 Me H CH.sub.2 OMe
SCH.sub.2 CCl.sub.3 SO.sub.2 Me H CH.sub.2 OMe Y21 SO.sub.2 Me H
CH.sub.2 OMe SPh SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me H CH.sub.2 OMe SCH.sub.2 CH.sub.2 OEt SO.sub.2 Me H
CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe
Y22 SO.sub.2 Me H CH.sub.2 OMe S(O)CH.sub.2 CHCH.sub.2 SO.sub.2 Me
H CH.sub.2 OMe S(O)CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe
S(O)CH.sub.2 C CH SO.sub.2 Me H CH.sub.2 OMe S(O)CH.sub.2 CH.sub.2
Cl SO.sub.2 Me H CH.sub.2 OMe Y23 SO.sub.2 Me H CH.sub.2 OMe
SO.sub.2 CH.sub.2 CHCH.sub.2 SO.sub.2 Me H CH.sub.2 OMe SO.sub.2
CH.sub.2 CHCMe.sub.2 SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2
CCH SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 CH.sub.2 CF.sub.3 SO.sub.2
Me H CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 Cl SO.sub.2 Me H
CH.sub.2 OMe Y24 SO.sub.2 Me H CH.sub.2 OMe SO.sub.2 Ph SO.sub.2 Me
H CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe SO.sub.2 Me H
CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OEt SO.sub.2 Me H CH.sub.2
OMe SO.sub.2 CH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me H CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OEt SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe
OCHMeCH.sub.2 OMe SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2
CH.sub.2 SMe
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Me
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 S(O)Pr-i
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2
Pr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2
OPr-i SO.sub.2 Me CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SOMe
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2
Me SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SPr-i
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2
Pr-i SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OMe
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2 CH.sub.2 OPr-i
SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2
OMe SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OPr-i SO.sub.2 Me CH.sub.2 COPh CH.sub.2 OMe OCH.sub.2
CH.sub.2 OMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OEt Cl H CH.sub.2
OMe OCH.sub.2 CH.sub.2 OPr-i Cl H CH.sub.2 OMe OCHMeCH.sub.2 OMe Cl
H CH.sub.2 OMe OCH.sub.2 COOMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2
SMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl H CH.sub. 2
OMe SCH.sub.2 CH.sub.2 OMe Cl H CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl H CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2
Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 Ph CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SOMe Cl CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2
CH.sub.2 SO.sub.2 Me Cl CH.sub.2 Ph CH.sub.2 OMe SCH.sub.2 CH.sub.2
OMe Cl CH.sub.2 Ph CH.sub.2 OMe SO.sub.2 CH.sub.2 CH.sub.2 OMe Cl
CH.sub.2 Ph CH.sub.2 OMe OCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh
CH.sub.2 OMe OCH.sub.2 CH.sub.2 SMe Cl CH.sub.2 COPh CH.sub.2 OMe
OCH.sub.2 CH.sub.2 SO.sub.2 Me Cl CH.sub.2 COPh CH.sub.2 OMe
SCH.sub.2 CH.sub.2 OMe Cl CH.sub.2 COPh CH.sub.2 OMe SCH.sub.2
CH.sub.2 OEt Cl CH.sub.2 COPh CH.sub.2 OMe SO.sub.2 CH.sub.2
CH.sub.2 OMe Cl CH.sub.2 COPh
______________________________________
When the compound of the present invention is to be used as an
agricultural or horticultural herbicide, it is usually mixed with a
suitable carrier, for instance, a solid carrier such as clay, talc,
bentonite or diatomaceous earth, or a liquid carrier such as water,
an alcohol (such as benzene, toluene or xylene), a chlorinated
hydrocarbon, an ether, a ketone, an ester (such as ethyl acetate)
or an acid amide (such as dimethylformamide). If desired, an
emulsifier, a dispersing agent, a suspending agent, a penetrating
agent, a spreader or a stabilizer may be added to prepare an
optional formulation such as a liquid formulation, an emulsifiable
concentrate, a wettable powder, a dust, a granule or a
flowable.
Further, if desired, other herbicides, various insecticides,
bacteriocides, plant regulating agents or synergism agents may be
combined at the time of the preparation of the formulations or at
the time of the application of the herbicides.
As other herbicides to be combined with the herbicide of the
present invention, there may be mentioned, for instance, compounds
disclosed in Farm Chemicals Handbook, the 73rd Edition (1987).
Among them, there may be mentioned, for example, atrazine,
cyanazine, alachlor, metolachlor, EPTC, 2,4-D, butylate, dicamba,
bromoxynil, tridiphane, isoproturon, chlortoluron, triallate,
difluphenican, diclofop methyl, diphenzoquat, imazamethabenz
methyl, ioxynil, methabenzthazuron, fluroxypil, chlorsulfuron and
N-[(4,6-di(difluoromethoxy)pyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonyl
benzenesulfonamide.
N-[(4,6-dimethoxypyrimidin-2-yl)-aminocarbonyl]-3-chloro-4-methoxycarbonyl
-1-methylpyrazole-5-sulfonamide or
N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-3-bromo-4-methoxycarbonyl-1
-methylpyrazole-5sulfonamide as disclosed in U.S. Pat. No.
4,668,277, or
N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-3-dimethylaminocarbonylpyri
dine-2-sulfonamide as disclosed in Japanese Unexamined Patent
Publication No. 223180/1987 may also be combined with the herbicide
of the present invention.
The dose varies depending upon the application site, the season for
application, the method for application, the type of the crop
plant, etc. In general, however, the dose is usually within a range
of from 0.001 to 10 kg per hectare as the amount of the active
ingredient.
Now, Formulation Examples of the herbicides containing the
compounds of the present inveniton as active ingredients, will be
given. However, it should be understood that the present invention
is by no means restricted to such specific Examples. In the
following Formulation Examples, "parts" means "parts by
weight".
FORMULATION EXAMPLE 1
Wettable powder
______________________________________ Compound No. 1 of the
present invention 60 parts Zeeklite PFP (tradename for a
kaolin-type 33 parts clay, manufactured by Zeeklite Industries,
Co., Ltd.) Sorpol 5039 (tradename for a mixture of a 5 parts
nonionic surfactant and an anionic surfactant, manufactured by Toho
Chemical Co., Ltd.) Carplex (tradename for a coagulation- 2 parts
preventing agent composed of a mixture of a surfactant and fine
silica powder, manufactured by Shionogi Pharmaceutical Co., Ltd.)
______________________________________
The above ingredients are homogeneously pulverized and mixed to
form a wettable powder.
FORMULATION EXAMPLE 2
Emulsifiable concentrate
______________________________________ Compound No. 1 of the
present invention 1.5 parts Xylene 78.5 parts N,N-dimethylformamide
15 parts Sorpol 2680 (tradename for a mixture of a 5 parts nonionic
surfactant and an anionic surfactant, manufactured by Toho Chemical
Co., Ltd.) ______________________________________
The above ingredients are homogeneously mixed to form an
emulsifiable concentrate.
FORMULATION EXAMPLE 3
Flowable
______________________________________ Compound No. 1 of the
present invention 40 parts Agrizole B-710 (tradename for a nonionic
10 parts surfactant, manufactured by Kao Corporation) Runox 1000C
(tradename for an anionic 0.5 part surfactant, manufactured by Toho
Chemical Co., Ltd.) 1% Rodopol water (tradename for a thickner, 20
parts manufactured by Rhone-Poulenc) Water 29.5 parts
______________________________________
The above ingredients are homogeneously mixed to form a
flowable.
FORMULATION EXAMPLE 4
Liquid formulation
______________________________________ Sodium salt of Compound No 1
of the 30 parts present invention Nippol (tradename for a nonionic
10 parts surfactant, manufactured by Nissan Chemical Industries
Ltd.) Water 60 parts ______________________________________
The above ingredients are homogeneously mixed to obtain a liquid
formulation.
FORMULATION EXAMPLE 5
Liquid formulation
______________________________________ Potassium salt of Compound
No. 1 of the 30 parts present invention Nippol (tradename for a
nonionic 10 parts surfactant, manufactured by Nissan Chemical
Industries Ltd.) Water 60 parts
______________________________________
The above ingredients are homogeneously mixed to obtain a liquid
formulation.
FORMULATION EXAMPLE 6
Liquid formulation
______________________________________ Calcium salt of Compound No.
1 of the 30 parts present invention Nippol (tradename for a
nonionic 10 parts surfactant, manufactured by Nissan Chemical
Industries Ltd.) Water 60 parts
______________________________________
The above ingredients are homogeneously mixed to obtain a liquid
formulation.
FORMULATION EXAMPLE 7
Liquid formulation
______________________________________ Isopropylamine salt of
Compound No. 1 of the 10 parts present invention Sorpol W-150
(tradename for a nonionic 10 parts surfactant, manufactured by Toho
Chemical Co., Ltd.) Water 80 parts
______________________________________
The above ingredients are homogeneously mixed to form a liquid
formulation.
In their use, the above wettable powder, emulsifiable concentrates,
flowables or liquid formulations are diluted with water from 50 to
1,000 times and applied so that the respective active ingredients
will be from 0.001 to 5 kg per hectare.
The compounds of the present invention are applicable not only to
agricultural and horticultural fields such as upland fields, paddy
fields and orchards, but also to non-agricultural fields such as
athletic fields, vacant fields and railway sides for the control of
various weeds. The dose in their application varies depending upon
the application site, the season for application, the type of crop
plants, etc. However, it is usually within a range of from 0.001 to
5 kg per hectare.
Now, the herbicidal activities of the compounds of the present
invention will be described with respect to specific Test
Examples.
TEST EXAMPLE 1:
Test on the herbicidal effects in soil treatment
A plastic box having a length of 15 cm, a width of 22 cm and a
depth of 6 cm was filled with a sterilized diluvium soil, and seeds
of Echinochloa crus-galli, Setaria viridis, Eleusine indica,
Digitaria adscendens, Panicum dichotomiflorum, Abutilon
theophrasti, Amaranthus lividus, Polygonum longisetum and Zea mays
were sown, and tubers of Cyperus esculentus were further planted.
The soil was covered thereon in the thickness of about 1.5 cm, and
then a herbicide solution was applied onto the surface of the soil
uniformly so that the active ingredient was distributed at a
predetermined concentration. The herbicide solution was prepared by
diluting the wettable powder, the emulsifiable concentrate, the
liquid formulation or the flowable as described in the foregoing
Formulation Examples with water and applied onto the entire soil
surface by means of a small spray. Three weeks after the
application of the herbicidal solution, the herbicidal effects
against each weed were determined on the basis of the following
standard ratings. The results thereby obtained are shown in Table
9. The Compound Nos. correspond to the Compound Nos. in Table
2.
Standard ratings
5: Growth control rate of more than 90% (almost completely
withered)
4: Growth control rate of from 70 to 90%
3: Growth control rate of from 40 to 70%
2: Growth control rate of from 20 to 40%
1: Growth control rate of from 5 to 20%
0: Growth control rate of less than 5% (almost non-effective)
The above growth control rates were calculated by the following
equation: ##EQU1## where T: Weight of the weed growth above the
soil surface of the treated area
N: Weight of the weed growth above the soil surface of the
non-treated area
TEST EXAMPLE 2:
Test 1 on the herbicidal effects in foliage treatment
A plastic box having a length of 15 cm, a width of 22 cm and a
depth of 6 cm was filled with a sterilized diluvium soil, and seeds
of Echinochloa crus-galli, Setaria viridis, Eleusine indica,
Digitaria adscendens, Panicum dichotomiflorum, Xanthium
strumatirum, Abutilon theophrasti, Amaranthus lividus, Polygonum
longisetum and Zea mays were spot-wisely sown, and tubers of
Cyperus esculentus were further planted. Then, the soil was covered
thereon in a thickness of about 1.5 cm. When the various weeds and
crop plant grew to the 2 or 3 leaf stage, a herbicidal solution was
uniformly sprayed on the foliages so that the active ingredient was
applied in a predetermined concentration.
The herbicidal solution was prepared by diluting the wettable
powder, the emulsifiable concentrate, the liquid formulation or the
flowable as described in the above Formulation Examples with water
and applied onto the entire surface of the foliages of the weeds
and the crop plants by a small spray. Two weeks after the
application of the herbicide solution, the herbicidal effects
against each weed and Zea mays were determined on the basis of the
standard ratings described in Test Example 1. The results are shown
in Table 10. The Compound Nos. in Table 10 correspond to the
Compound Nos. in Table 2.
TEST EXAMPLE 3
Test 2 on the herbicidal effects in foliage treatment
A plastic box having a length of 15 cm, a width of 22 cm and a
depth of 6 cm was filled with a sterilized diluvium soil, and seeds
of Veronica persica, Stellaria media, Galium spurium, Matricaria
matricarioides, Polygonum persicaria, Lamium purpureum, Solanum
nigrum and Triticum aestivum were spot-wisely sown. Then, the soil
was covered thereon in a thickness of about 1.5 cm. When the
various weeds and crop plant grew to the 2 or 3 leaf atage, a
herbicidal solution was uniformly sprayed on the foliages so that
the active ingredient was applied in a predetermined
concentration.
The herbicidal solution was prepared by diluting the wettable
powder, the emulsifiable concentrate, the liquid formulation or the
flowable as described in the above Formulation Examples with water
and applied onto the entire surface of the foliages of the weeds
and Triticum aestivum by a small spray. Two weeks after the
application of the herbicide solution, the herbicidal effects
against each weed and Triticum aestivum were determined on the
basis of the standard ratings described in Test Example 1 The
results are shown in Table 11. The Compound Nos in Table 11
correspond to Compound Nos. in Table 2.
In Tables 9, 10 and 11, the following abbreviations are used.
Dose: Dose of active ingredient (g/are)
EC: Echinochloa crus-galli (barnyardgrass)
SE: Setaria viridis (green foxtail)
EL: Eleusine indica (goosegrass)
DI: Digitaria adscendens (large crabgrass)
PA: Panicum dichotomiflorum (fall panicum)
AB: Abutilon theophrasti (velvet leaf)
AM: Amaranthus lividus (livid amaranth)
PO: Polygonum longisetum (persicaria blumei gross)
XA: Xanthium strumarium (cocklebur)
CY: Cyperus esculentus (yellow nutsedge)
ZE: Zea mays (corn)
VE: Veronica persia (birdseye speedweell)
ST: Stellaria media (chickweed)
GA: Galium spurium (catchweed)
MA: Matricaria matricarioides (pineappleweed)
PP: Polygonum persicaria (ladysthumb)
LA: Lamium purpureum (red deadnettle)
SO: Solanum nigrum (black nigthshade)
TR: Triticum aestivum (wheat)
TABLE 9
__________________________________________________________________________
Compound Dose No. g/are EC SE EL DI PA AB AM PO CY ZE
__________________________________________________________________________
1 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 0
4 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 0
6 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 0
7 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 0
11 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5
0 18 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5
5 0 19 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5
5 5 0 20 1 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5
5 5 5 0 Compara- 4 3 1 3 3 1 4 5 5 0 0 tive 8 4 2 4 4 2 5 5 5 0 0
Compound 16 5 3 5 5 3 5 5 5 1 1 Compara- 4 5 5 5 5 5 1 1 1 2 0 tive
8 5 5 5 5 5 2 2 2 3 0 Compound 16 5 5 5 5 5 3 3 3 4 1 B
__________________________________________________________________________
TABLE 10
__________________________________________________________________________
Compound Dose No. g/are EC SE EL DI PA AB AM PO XA CY ZE
__________________________________________________________________________
1 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5
5 5 0 4 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5
5 5 5 5 5 0 6 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 4 5 5
5 5 5 5 5 5 5 5 0 7 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0
4 5 5 5 5 5 5 5 5 5 5 0 11 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5 5
5 5 5 0 4 5 5 5 5 5 5 5 5 5 5 0 18 1 5 5 5 5 5 5 5 5 5 5 0 2 5 5 5
5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 5 0 19 1 5 5 5 5 5 5 5 5 5 5 0
2 5 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 5 0 20 1 5 5 5 5 5 5 5
5 5 5 0 2 5 5 5 5 5 5 5 5 5 5 0 4 5 5 5 5 5 5 5 5 5 5 0 Compara- 4
3 1 2 3 0 3 5 5 4 0 0 tive 8 4 2 3 4 1 5 5 5 5 0 1 Compound 16 4 2
3 4 1 5 5 5 5 0 1 Compara- 4 4 3 3 4 3 0 2 2 0 1 0 tive 8 4 4 4 4 4
1 3 3 1 2 1 Compound 16 5 5 5 5 5 2 4 4 2 3 2 B
__________________________________________________________________________
TABLE 11 ______________________________________ Com- pound Dose No.
g/are VE ST GA MA PP LA SO TR
______________________________________ 1 0.5 5 5 5 5 5 5 5 0 1 5 5
5 5 5 5 5 0 2 5 5 5 5 5 5 5 0 7 0.5 5 5 5 5 5 5 5 0 1 5 5 5 5 5 5 5
0 2 5 5 5 5 5 5 5 0 11 0.5 5 5 5 5 5 5 5 0 1 5 5 5 5 5 5 5 0 2 5 5
5 5 5 5 5 0 18 0.5 5 5 5 5 5 5 5 0 1 5 5 5 5 5 5 5 0 2 5 5 5 5 5 5
5 0 Compar- 1 4 4 3 2 4 2 4 0 ative 2 5 5 4 4 5 4 5 1 Com- pound C
______________________________________
In Tables 9 and 10, the Comparative Compounds are as follows:
##STR40##
In Table 11, the Comparative Compound is as follows:
* * * * *