| Summary: | Chiral benzothiazepines constitute the core structures of many foremost pharmaceuticals with diverse biological activities endowed by their unique scaffolds, which poses a great challenge to organic chemists and pharmaceutical researchers. This review provides a concise overview for the asymmetric synthesis of chiral benzothiazepine derivatives, focusing on advances in asymmetric catalysis, including metal catalysis, small-molecule organocatalysis and enzymatic catalysis. The catalytic asymmetric reactions, involving asymmetric epoxidation, reduction, dihydroxylation, hydrogenation, aldol reaction and other sulfa-Michael addition, have emerged as powerful strategies for the rapid construction of chiral benzothiazepine through single or multistep reactions. The booming asymmetric synthetic methodology affords us instructive clues for the highly efficient preparation of chiral benzothiazepines, facilitating their large-scale preparation and diversity-oriented synthesis.
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