Copper-Catalyzed Coupling of Alkynes and Amines for the Synthesis of Propargyl Amines in the Presence of PhI(OAc)₂

Abstract

In the presence of iodobenzene diacetate (PhI(OAc) 2 ), a new CuBr catalyzed coupling reaction of alkynes and amines for the synthesis of propargyl amines was developed. When terminal alkynes, PhI(OAc) 2 , and amines were reacted in CH 3 CN at 70 ℃ for 3 h under N 2 atmosphere and in the presence of CuBr, the desired propargyl amines were obtained in good yields. Furthermore, no matter aromatic or aliphatic alkynes, were all found to tolerate the reaction conditions. To the best of our knowledge, it is the first time that PhI(OAc) 2 has been used for the synthesis of propargyl amines in one-pot operation from alkynes and amines.