PROCESS FOR THE PREPARATION OF 1,4-BENZODIAZEPINE DERIVATIVES

摘要

PROCESS FOR THE PREPARATION OF 1,4-BENZODIAZEPINE DERIVATIVES A 1,4-benzodiazepine derivative, or a pharmaceutically acceptable acid salt thereof, of the formula, wherein R1 is hydrogen, halogen, nitro or trifluoromethyl; R2 and R3 are independently hydrogen, halogen, lower alkyl or trifluoromethyl; R4 is lower alkyl, alkenyl, trihaloalkyl, alkoxyalkyl, alkenyloxyalkyl, alkoxyalkoxyalkyl, alkanoyloxyalkyl, cycloalkylalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl or a group of the formula in which R6 and R7 are independently lower alkyl, and n is an integer of 1 to 4; and R5 is hydrogen or lower alkyl, is obtained by reacting a 1 benzophenone derivative of the formula, wherein R1, R2, R3 and R4 are as defined above, with a 2-isocyanatoacetyl chloride derivative of the formula wherein R5 is as defined above.