Cu(II)-Catalyzed, Site Selective Sulfoximination to Indole and Indolines via Dual C-H/N-H Activation.

A copper-catalyzed protocol furnishing -arylated sulfoximines has been developed via dual N-H/C-H activation. Arylalkyl- and less reactive diarylsulfoximines were efficiently coupled with privileged scaffolds like indolines, indoles, and -Ar-7-azaindoles. Sulfoximines based on medicinally relevant scaffolds (phenothiazine, dibenzothiophene, thioxanthenone) were also well tolerated. Detailed mechanistic studies indicate that the deprotometalation and protodemetalation step is the reversible step.