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Chemical properties of 2,3-dihydro-1H-1,5-benzodiazepinone-2 derivatives – a review

Aleksandr A. Gaponov, Аndrey А. Anishchenko


Condensed heterocyclic systems with two nitrogen atoms in the seven-membered ring – benzodiazepines and their derivatives – are interesting and important objects from both theoretical and applied point of view. They attract a lot of attention due to their potent and diverse biological activities. These compounds include numerous tranquilizers, sedatives, analgesics, as well as anticonvulsant, anti-inflammatory and anti-tumor agents. The presence of several reactive centers in 1,5-benzodiazepines leads to a variety of reactions with both electrophilic and nucleophilic agents. The first part of this review covers electrophilic substitution of 2,3-dihydro-1H-1,5-benzodiazepin-2-ones (nitration, halogenation, alkylation, acylation, formylation, etc.) The data shows that the reaction outcome is determined by the nature of both the substrate and the electrophilic agent, as well as by the reaction conditions: temperature, time, and solvent. 


1,5-dihydrobenzodiazepinone-2; biological activity; reaction of electrophilic substitution; reaction with nucleophilic reagents


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