Fused 1,5-benzothiazepines from o-aminothiophenol and its derivatives as versatile synthons

Abstract

This review describes the reactions of o-aminothiophenol and its derivatives as building blocks for the synthesis of polyfunctionalised 1,5-benzothiazipines with pharmacological interest. Annelated 1,5-benzothiazipines were prepared by a cyclocondensation reaction of o-aminothiophenol and its derivatives with carbonyl and other functionalities. In case of carbonyl function this reaction takes place by a nucleophilic addition, followed by cyclisation concomitant with elimination of water. The objective of this survey is to provide a comprehensive account of the synthesis of various 1,5-benzothiazepines derivatives and their potential to develop better chemotherapeutic agents.