Process for the manufacture of benzodiazepine derivatives

Details Process for the manufacture of benzodiazepine derivatives Process for the manufacture of benzodiazepine derivatives

C - Chemistry, Metallurgy

07

D

260/240.4

C07D 243/28 (2006.01) C07D 401/04 (2006.01)

Patent

CA 1055491

Abstract Benzodiazepine derivatives of formula Image I wherein R signifies hydrogen or alkyl, R1 signifies hydrogen, halogen or trifluoromethyl and R2 signifies phenyl, halophenyl or pyridyl, and 4-oxides thereof are prepared by a novel process which comprises reacting a benzophenone of the general formula Image II wherein R, R1 and R2 are as defined above with a nitroacetic acid halide, reducing the abtained nitro- acetyl compound of the general formula Image III wherein R, R1 and R2 are as defined above to the corresponding hydroxylamine or amine derivative and cyclizing the product thus obtained. Benzodiazepines of formula I and 4-oxides thereof are known compounds which are known to be useful as sedatives, anticonvulsants and muscle relaxants.

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