STEREOSELECTIVE PROCESS FOR PRODUCING 5-ARYL-8,9- DIHYDRO-7H- 1,3-DIOXOLO 4,5-h-2,3- BENZODIAZEPINE DERIVATIVES AND THE INTERMEDIATE 5-AROYL- 6-(2-SUBSTITUTED ALKYL)-1,3- BENZODIOXOLE HYDRAZONE DERIVATIVES THEREFOR

摘要

A process for preparing a compound of the formula wherein Aryl is an unsubstituted or substituted aryl group; and R is hydrogen or a C1-C10 alkyl; and X is hydrogen, C1-C10 alkyl, acyl, aryl as hereinbefore defined, carboxyl or a substituted derivative thereof, or a protecting group, or a pharmaceutically acceptable salt thereof, said process comprising cyclising a compound of the formula 468 כ" ג בתמוז התש" ס - July 26, 2000 wherein Z represents a leaving atom or group, to afford a compound having the general formula I, whereafter, if desired, converting the compound of formula I into another compound of formula I and/or forming a pharmaceutically acceptable salt. Claimed as new are compounds of the formula wherein Aryl is an unsubstituted or substituted aryl group; R is hydrogen or a C1-C10 alkyl; X is hydrogen, C1-C10 alkyl, acyl, aryl, carboxyl or a substituted derivative thereof, or a protecting group; and Z is a hydroxyl group or a leaving atom or group, or a salt thereof.