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

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