Benzodiazepines - from benzophenones and protected diamines or-aminoides followed by cyclisation

摘要

Cpds. (I) (where R1 is H, alkyl, alkaryl or aryl; R2 and R3 are H, halogen, alkyl, alkaryl, alkoxy, NO2, SO3H or SO2NH2; Y is CO or CH2), are prepd. by reacting the appropriate halobenzophenone with R1NAYCH2NZ (where Z is a blocking gp.), treating the prod. with N2H4, to regenerate the prim. amine, which reacts with the CO gp. to give a benzodiazepine cpd.