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This privileged scaffold exhibits a diversity of biological activities, including antimicrobial, antibacterial, anti\u2010epileptic, anti\u2010HIV, antidepressant, antithrombotic and anticancer properties. Its important pharmacological potential renders research into the development of new and efficient synthetic methods of high relevance. In the first part of this review, an overview of different synthetic approaches toward 1,5\u2010benzothiazepane and its derivatives is provided, ranging from established protocols to recent (enantioselective) methods that promote sustainability. 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