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

A copper-catalyzed protocol furnishing N-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 N-Ar-7-azaindoles. Sulfoximines based on medicinally relevant scaffolds (phenothiazine, dibenzothiophene, thioxanthenone) were also well tolerated. Detailed mechanistic studies indicate that the depro-tometalation and protodemetalation step is the reversible step.

Automated summary

A copper-catalyzed method for the synthesis of N-arylated sulfoximines via dual N-H/C-H activation has been developed. This method shows good compatibility with various commonly used functional groups as well as medicinally relevant scaffolds.