Copper-Catalyzed Highly Efficient Acetylene-Mannich Reaction of Secondary Amines,Paraformaldehyde and Terminal Alkynes

摘要

A Cu(0)-catalyzed multicomponent reaction of tetrahydroisoquinolines (THIQ),paraformaldehyde and terminal alkynes to form propargylamines is developed.This protocol worked well for other secondary amines too.Acetylene-Mannich products were obtained in high yields (up to 98% yields).This acetylene-Mannich reaction is operationally simple,scalable and exhibits high functional-group tolerance.