Process for the preparation of imidazobenzodiazepines

C - Chemistry – Metallurgy – 07 – D

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260/239.4

C07D 487/04 (2006.01) C07D 243/16 (2006.01) C07D 498/04 (2006.01)

Patent

CA 1126270

RAN 4008/304 ABSTRACT Imidazobenzodiazepines of the formula Image I wherein X represents hydrogen, halogen, nitro or trifluoromethyl, Y represents hydrogen, halogen or trifluoromethyl, R1 represents hydrogen, lower alkyl or aryl and n represents the integer 0 or 1, and pharmaceutically acceptable acid addition salts there- of are prepared by a novel process which comprises reac- ting a compound of formula Image II wherein R represents hydrogen or lower alkyl and X, Y and n have the meaning indicated above, with an aldehyde of the formula R1-CHO III wherein R1 has the meaning indicated above, or converting a compound of formula Image or Image IV V wherein X, Y and n have the meaning indicated above, into the corresponding compound of formula I by treatment with an acid, and respectively, an acid or a base, and if desired, converting a compound thus obtained into a pharmaceutically acceptable acid addition salt thereof. The compounds of formula I are known and useful as sedatives, anxiolytics, muscle relaxants and anticonvul- sants.

356925

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