Alumina-supported phosphorus pentoxide was found to be an efficient reagent for the synthesis of 1,5-benzodiazepine derivatives from phenylenediamine and ketones in the solvent-free condition under microwave irradiation. This method is an easy, rapid, and high-yielding reaction for the synthesis of 1, 5-bezodiazepines.Heterocyclic compounds hold a special place among pharmaceutically important natural and synthetic materials. The remarkable ability of heterocyclic nuclei to serve both as biomimetics and active pharmacophores has largely been contributed to their unique value as traditional key elements of numerous drugs. 1 The benzodiazepine nucleus is a well-studied traditional pharmacophoric scaffold that has emerged as a core structural unit of various sedative hypnotic, muscle relaxant, anxiolytic, antistaminic, and anticonvulsant agents. 2 Although the first benzodiazepine was introduced as a drug nearly 30 years ago the research in this area is still very active and is directed toward the synthesis of compounds of enhanced pharmacological activity. Several methods, not generally applicable, have been reported in the literature for synthesis of 1,5-benzodiazepines. 3-7 Unfortunately, many of these processes suffer limitations, such as drastic reaction conditions, low yields, tedious work-up procedures and cooccurrence of several side reactions. Recently we found that the mixture of magnesium oxide with phosphorus oxychloride is a new reagent for the synthesis of 1,5-benzodiazepines. 8 However, treatment
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