Synthesis 2013; 45(7): 952-958
DOI: 10.1055/s-0032-1316862
paper
© Georg Thieme Verlag Stuttgart · New York

Efficient One-Pot Synthesis of Propargylamines from Mannich Bases through a Retro-Mannich-Type Fragmentation

Yefeng Zhu
School of Chemical Engineering, Nanjing University of Science and Technology, Nanjing 210094, P. R. of China   Fax: +86(25)84317078   Email: ywei@mail.njust.edu.cn
,
Huishuang Zhao
School of Chemical Engineering, Nanjing University of Science and Technology, Nanjing 210094, P. R. of China   Fax: +86(25)84317078   Email: ywei@mail.njust.edu.cn
,
Yunyang Wei*
School of Chemical Engineering, Nanjing University of Science and Technology, Nanjing 210094, P. R. of China   Fax: +86(25)84317078   Email: ywei@mail.njust.edu.cn
› Author Affiliations
Further Information

Publication History

Received: 16 January 2013

Accepted after revision: 06 February 2013

Publication Date:
27 February 2013 (online)


Abstract

An efficient one-pot synthesis of propargylamines is achieved by copper-catalyzed coupling of phenylacetylenes with Mannich bases through a chlorine(1+) or bromine(1+) ion-initiated retro-Mannich-type fragmentation under mild conditions. The Mannich bases are easily prepared from an electron-rich phenol, formaldehyde, and an amine. The protocol provides an appealing alternative for the construction of propargylamines by a simple one-pot procedure.