The 1,4-diazepine and 1,4-benzodiazepine structures have been found in the naturally occurring products and are significant biomolecules in medicinal chemistry with a wide range of biological and pharmacological activities such as antibiotic, [1] antimalarial, [2] anti-HIV, [3] and anticancer.[4] The benzodiazepines are also the most widely prescribed minor tranquilizers in current use, and they are known to act on the central nervous system. Therefore, benzodiazepines are an important class of psychotherapeutic compounds. [5] Dweu e tsoy tnhteh ewsiidzeesdp revaadri obuioslo gdicearli vaacttiivveitsie s ooff fubseendz hoe[ete]pryorcayzcolilco [s5y',s1te':2m,3s,]p iny rtihmisid sot[u5d,4y-, b][1,4]diazepine as a novel heterocyclic system. In this one-pot protocol, the desired products (3a-h) were obtained through the cyclocondensation of diverse synthesized 2-amino-N-alkylbenzamides (1a-h) with 6-bromo-7-chloro-2-(ethylthio)-5- methylpyrazolo[1,5-a]pyrimidine-3-carbonitrile (2) in the presence of K2CO3 in DMF. The true regioisomers of heterocyclization were also investigated.

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