Method for the preparation of 4-phenyl-1,3-benzodiazepines and precursors thereof

摘要

A compound of the formula <IMAGE> (II) is prepared by reacting an N-acylated-o-toluidine of the formula <IMAGE> (III) with n-alkyllithium to form a dilithio intermediate of the formula <IMAGE> (IV) which can then be quenched with N-benzylidenemethylamine to form compound II. Hydrolysis of compound(II)yields the free base <IMAGE> (V) or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.