摘要:
The present invention concerns compounds of formula (A1)(A2)N—R1 (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula
摘要:
The present invention concerns compounds of formula (A1)(A2)N—R1 (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula
摘要:
This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, provided that when Q is halo then Z is N; or when Q is polyhaloC1-6alkyl then Y is hydrogen or C1-6alkyl; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
摘要:
A novel process for the preparation of compounds of the formula ##STR1## with cis or trans structure in racemic or optically active form wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl of 6 to 12 carbon atoms comprising reacting an optically active isomer, or racemate of the formula ##STR2## wherein R has the above definition and the way line indicates Z or E geometry with a gem-dimethyl cyclopropanation agent if there is Z geometry to obtain a compound of the formula ##STR3## or if the geometry is E with a gem-dimethyl cyclopropanation agent other than isopropylidene triphenyl phosphorane to obtain a compound of the formula ##STR4## wherein R has the above definition and the cyclopropane ring has the trans configuration and either hydrolyzing the compound of formula III or IIIa to obtain a compound of the formula ##STR5## and then cleaving the 4,5 bond to obtain the corresponding compound of formula I or simultaneously cleaving the 4,5 bond and hydrolyzing the dioxolane group to obtain the corresponding compound of formula I and novel intermediates.
摘要:
A novel process for the preparation of esters of 2,2-dimethyl-cyclopropane-1,3-dicarboxylic acids in their optically active forms having a cis or trans configuration I comprising salifying the monomethyl ester of (1RS,3SR) cis 2,2-dimethyl-cyclopropane-1,3-dicarboxylic acid with d or l .alpha.-methyl-benzylamine, recovering the crystallized salt formed, dissolving the said salt in water, treating the solution with a mineral base and then with an acid to obtain either the monomethyl ester of (1R,3S) cis 2,2-dimethyl-cyclopropane-1,3-dicarboxylic acid I or its (1S,3R) cis isomer depending on whether d or l .alpha.-methyl-benzylamine, respectively was used, if desired, reacting the latter cis compound with a strong base to isomerize the monomethyl ester to the monomethyl ester of (1S,3S) trans 2,2-dimethyl-cyclopropane-1,3-dicarboxylic acid I or (1R,3R) trans isomer, respectively, or reacting the latter cis compound with a tert-butyl esterification agent to obtain a compound of (1S,3R) configuration of the formula ##STR1## or a compound of (1R,3S) configuration of the formula ##STR2## subjecting the said compound to selective hydrolysis to remove the methyl ester group to form a compound of the formula ##STR3## of (1S,3R) cis or (1R,3S) cis configuration, respectively and optionally subjecting the compound of formula I.sub.A to a strong isomerization base to obtain a compound of the formula ##STR4## of (1R,3R) trans or (1S,3S) trans configuration which is a useful intermediate for the preparation of pesticidal compositions.
摘要:
Novel methyl esters of cis or trans configuration in their optically active form of the formual ##STR1## which are useful as intermediates for the preparation of pesticidal compounds and a process for their preparation and intermediates.
摘要:
The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula
摘要:
A novel process for the preparation of alkyl esters of dl-trans chrysanthemic acid of the formula ##STR1## wherein R is alkyl of 1 to 6 carbon atoms comprising reacting in the presence of a strong base an alkyl 4-oxo-2E-butenoate of the formula ##STR2## with at least about 2 molar equivalents of a triphenyl isopropyl phosphonium halide which uses easily accessible starting materials.