Brønsted Base-Switched Selective Mono- and Dithiolation of Benzamides via Copper Catalysis

J Org Chem. 2019 Aug 16;84(16):10490-10500. doi: 10.1021/acs.joc.9b01237. Epub 2019 Aug 2.

Abstract

A versatile protocol for the direct thiolation of an inert sp2 C-H bond is presented via a catalytic amount of copper catalysis, by switching related Brønsted bases and regulating the reaction time, and the corresponding mono- and dithiolation products can be obtained selectively in moderate to good yields. The reaction exhibits a relatively broad substrate scope and a good functional group tolerance, even with different heterocyclic amides and alkyl thiols.