Direct thiolation of aza-heteroaromatic N-oxides with disulfides via copper-catalyzed regioselective C–H bond activation

Abstract

A novel and regioselective thiolation reaction of aza-heteroaromatic N-oxides with disulfides via copper catalyzed C–H activation has been developed. The desired thioethers and selenide ethers were isolated in up to 90% yield and feature a very broad substrate scope. In addition, the C(sp³)–H bonds of methyl-substituted aza-heteroaromatic compounds were also tolerated in this reaction and the corresponding dithioacetal products were obtained in moderate to good yields.