Quat. ammonium derivs. of (1,4)-benzodiazepinones prepn. - with CNS activity

摘要

Prepn. of 1,4-benzodiazepin-2-one quat. ammonium derivs derivs. of formula (I) comprises reacting the corresp. 3- halo-1,4-benzodiazepin-2-one derivs. of formula (I; -N circled positive A X circled negative is halogen) with a tert. amine of formula NA (III). In the formulae, R1 is H, halogen, or CF3; R2 is H or 1-4C alkyl; Ar is Ph or o-halophenyl; -NA circled positive is a quat. ammonium gp. (a) which contains a benzene ring and in which the free valence belongs to a non-heterocyclic N atom, or (b) in which the free valence belongs to a heterocyclic N atom. In an example, 7-chlor-1-methyl-3-pyridinio-5-phenyl-2H-1,4-benzodiazepin-2-one chloride is prepd. from 3, 7-dichloro-1-methyl-5-phenyl-2H-1, 4-benzodiazepin-2-one and pyridine.