1 - (2 - Phthalic imido alkyl) - 6 - phenyl - 4h - s - triazolo bracket on 4,3 - a bracket to bracket on 1,4 bracket to - benzodiazepines and method for their preparation

摘要

There are prepared 1-(2-phthalimidoalkyl)-6-phenyl-4H-s-triazolo- [4,3-a][1,4]benzodiazepine of the formula IMAGE in which R denotes hydrogen or an alkyl radical having 1 to 2 carbon atoms, the ring A is unsubstituted or substituted by a fluorine, chlorine or bromine atom or a nitro or trifluoromethyl group and the ring B is unsubstituted or substituted by 1 chlorine atom or 1 or 2 fluorine atoms. These compounds are obtained by hydroxymethylating a corresponding 2(4H-1,2,4-triazol-4-yl)benzophenone with formaldehyde. The hydroxymethyl compound is then reacted with a halogenating agent to give the halomethyl compound and this is finally cyclised by treatment with ammonia or hexamethylenetetramine in an inert organic solvent. The resulting compounds can be used as starting substances for the preparation of tranquillisers.