Copper-Catalyzed One-Pot Synthesis of 2-Alkylidene-1,2,3,4-tetrahydropyrimidines

A one-pot synthesis of N-sulfonyl-2-alkylidene-1,2,3,4-tetrahydropyrimidines via a highly selective and copper-catalyzed multicomponent reaction of sulfonyl azides, terminal alkynes and alpha,beta-unsaturated imines has been developed. The alpha,beta-unsaturated imine substrates could be generated from amines and alpha,beta-unsaturated aldehydes in a one-pot process. The procedure is concise, general and efficient.