An efficient and facile one-pot synthesis of propargylamines by three-component coupling of aldehydes, amines, and alkynes via C-H activation catalyzed by NiCl2

NiCl2 was found to be a highly efficient and effective catalyst for the one-pot three-component (A(3)) coupling of aldehydes, amities, and alkynes to produce propargylamines in nearly quantitative yields. Structurally divergent aldehydes, amines, and alkynes were converted into the corresponding propargylamines. No co-catalyst or activator is needed and water is the only byproduct of this novel protocol. (C) 2010 Elsevier Ltd. All rights reserved.