Heterocycles containing the thiazepine moiety are important targets in synthetic and medicinal chemistry because this fragment is a key moiety in a wide number of natural and synthetic biologically active agents [1]. Among them, aryl- and heteroaryl-fused derivatives of this heterocycle represent an important group of compounds with interesting pharmaceutical properties. Like calcium channel antagonists, HIV-1 enzyme integraseand reverse transcriptaseinhibitors [2,3]. In this study we decided to synthesise a new fused pyrimidine ring system pyrimido[4′,5′:2,3][1,4]thiazepino[7,6-b]quinolineand to study its biological activities. For this purpose we first prepared compound (1) and (2) [4]. Treatment of (1a-d) with (2) in boiling N-N-di-methylformamide (DMF), in the presence of Et3N, afforded pyrimido[4,5:2,3][1,4]thiazepino[7,6-b]quinoline (3a-f) as the main products. Consequently, the biological activities of these compounds are also evaluated.

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