Copper-Catalyzed Asymmetric Synthesis of Heteroaryl Sulfoxide

The practical synthesis of heteroaryl chiral sulfoxides, which have wide applications in asymmetric catalysis and pharmaceutical chemistry, is significantly hindered by heteroatom-induced catalyst poisoning. To address this, we developed a general copper-catalyzed asymmetric cross-coupling of heteroaryl halides with sulfoxide precursors. This operationally simple method proceeds under mild conditions, tolerates a broad range of functional groups, and delivers diverse heteroaryl chiral sulfoxides in high yields with excellent enantioselectivity. The synthetic utility of this strategy is highlighted by the direct transformation of the products into other privileged scaffolds, such as chiral sulfoximines, underscoring its potential for late-stage diversification in drug discovery.