Transition-metal-free arene C–H functionalization for the synthesis of sulfoximines

Abstract

A transition-metal-free C–H functionalization method has been developed for the synthesis of aryl sulfoximines. This two-step protocol involves the 3,5-dimethyl-4-isoxazolyliodonium salt as an intermediate. The iodonium salt is obtained with high site selectivity from arenes via C–H activation, and is then converted into sulfoximines through a ligand coupling at the hypervalent iodine center with sulfinamides. The process is mild and does not require transition metals, enabling the late-stage incorporation of chiral sulfonimidoyl groups into drug candidates.