Regioselective Thiolation of Indoles with Sulfinyl Amides

Abstract

AbstractA mild, efficient and highly regioselective thiolation of indoles by sulfinyl amides via direct C−H functionalization is described. Sulfinyl amides could be reduced to thioethers and submitted as the thiolation reagents were developed. This reaction provides a useful method for the synthesis of 3‐indole thioethers and 2,3‐dithioindole derivatives. This mix‐and‐go approach also tolerates broad substrate scope and outstanding functional group compatibility. In addition, this preparation could be easily conducted on a gram scale with high efficiency.