Process for manufacture of imidazo benzodiazepine derivatives

Details Process for manufacture of imidazo benzodiazepine derivatives Process for manufacture of imidazo benzodiazepine derivatives

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01)

Patent

CA 2184802

The invention is concerned with a novel process for the manufacture of 4H-imidazo[1,5-a][1,4]benzodiazepine derivatives of general formula I (see formula I) wherein R1 signifies phenyl or mono- or disubstituted phenyl; R2 signifies hydrogen, halogen, nitro, cyano, trifluoromethyl or lower alkyl; R3 signifies hydrogen or lower alkyl; and R4 signifies hydrogen or lower alkyl and of pharmaceutically usable salts of these compounds by decarboxylating a 4H-imidazo[1,5-a][1,4]benzodiazepine- carboxylic acid of general formula II (see formula II) wherein R1, R2, R3 and R4 have the above significances, at elevated temperature and under elevated pressure in the presence of an organic solvent. The compounds of formula I and their pharmaceutically usable acid addition salts are known muscle relaxants, sedatives and anticonvulsants.

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