Process for the preparation of 1,4-benzodiazepine derivatives

Details Process for the preparation of 1,4-benzodiazepine derivatives Process for the preparation of 1,4-benzodiazepine derivatives

C - Chemistry, Metallurgy

07

D

260/240.2

C07D 243/28 (2006.01) C07D 243/24 (2006.01) A61K 31/55 (2006.01)

Patent

CA 1038382

PROCESS FOR THE PREPARATION OF 1,4-BENZODIAZEPINE DERIVATIVES ABSTRACT OF THE DISCLOSURE A 1,4-benzodiazepine derivative, or a pharmaceutically acceptable acid salt thereof, of the formula, Image wherein R1 is hydrogen, halogen, nitro or trifluoro- methyl; R2 and R3 are independently hydrogen, halogen, lower alkyl or trifluoromethyl; R4 is lower alkyl, alkenyl, trihaloalkyl, alkoxyalkyl, alkenyloxyalkyl, alkoxyalkoxy- alkyl, alkanoyloxyalkyl, cycloalkylalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl or a group of the formula Image in which R6 and R7 are independent- ly 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, Image wherein R1, R2, R3 and R4 are as defined above, with a 2-isocyanatoacetyl chloride derivative of the formula Image wherein R5 is as defined above.

220821

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