Enantioselective Synthesis of Chiral Sulfoxides via Copper-Catalyzed Asymmetric Alkyne-Azide Cycloaddition.

Chiral sulfoxide scaffolds widely exist in biologically active natural products, drugs, ligands, and catalysts. The synthesis of this kind of molecule has received a considerable amount of attention. Herein, we report a highly enantioselective copper-catalyzed asymmetric alkyne-azide cycloaddition synthesis of chiral sulfoxides via desymmetrization. The practicality and attractiveness of this method are exhibited utilizing readily available starting materials, mild reaction conditions, good enantioselectivity, and a broad substrate scope.