Three‐Component 1,2‐Methylamidation of Alkynes via Coordinating Activation Strategy

The selective functionalization of carbon-carbon triple bonds with methyl groups remains a challenging task. Herein, the successful development of a novel copper-catalyzed three-component 1,2-methylamidation of carbon-carbon triple bond is reported. The readily available coupling partners, picolinamides and alkynes with dicumyl peroxide, serve as both the methyl source and oxidant in this difunctional strategy to access methylated enamides; the substrate scope is broad, demonstrating good functional group compatibility. The synthetic utility of the reaction is also demonstrated through the 1,2-methylamidation of alkynes via late-stage functionalization of substrates bearing biologically relevant molecules.