Nickel catalyzed site selective C–H functionalization of α-aryl-thioamides

Abstract

A catalytic site selective intramolecular C–S bond forming reaction is demonstrated for the first time. The C–H bond functionalization of α-aryl-thioacetanilides was efficiently catalyzed by 2 mol% NiBr₂, resulting in valuable 2-aminobenzo[b]thiophenes in moderate to good yields. Furthermore, the selective sp² C–H bond functionalization over sp³ is exemplified.