5-(3'-AMINOPROP-1'-YL)-10-TRIFLUOROMETHOXY-5H-DIBENZ(B,F) AZEPINES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

1477635 Dibenzazepines RESEARCH INSTITUTE FOR MEDICINE & CHEMISTRY Inc 23 Aug 1974 [24 Aug 1973] 40242/73 Heading C2C Compounds of the general formula (RSP1,2/SP=H, alkyl; RSP3/SP = alkyl, optionally substituted, RSP4/SP=H or alkyl, optionally substituted, or NRSP3/SPRSP4/SP=heterocyclic group; the dibenzazepine nucleus optionally carrying one or more substituents selected from halogen, alkyl, alkoxy, alkylthio in position(s) 2, 3, 7 and/or 8 and their acid addition salts are prepared by (a) reacting the 5-unsubstituted compound or an alkali metal derivative thereof with (X=reactive ester radical; RSP7/SP = NRSP3/SPRSP4/SP or substituent convertible into or replaceable by such a group), followed by conversion of RSP7/SP to NRSP3/SPRSP4/SP if necessary, or (b) reducing the corresponding compound containing a keto group in the 1-position of the 5-substituent, optionally followed by salt formation in either case. The starting materials are prepared by reacting a 5 - acyl - 5H - dibenz[b,f]azepiae (obtained by acylation) with trifluoromethyl hypofluorite followed by dehydrofluorination and, if necessary, deacylation. The above compounds are antidepressants, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.