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 α,β‐unsaturated imines has been developed. The α,β‐unsaturated imine substrates could be generated from amines and α,β‐unsaturated aldehydes in a one‐pot process. The procedure is concise, general and efficient.