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Recent Advances in the Addition of Amide/Sulfonamide Bonds to Alkynes

Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, Chengdu University, 168 Hua Guan Road, Chengdu 610052, China
State Key Laboratory of Drug Research and CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China
University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing 100049, China
Author to whom correspondence should be addressed.
Academic Editor: Michal Szostak
Molecules 2019, 24(1), 164;
Received: 11 December 2018 / Revised: 27 December 2018 / Accepted: 27 December 2018 / Published: 4 January 2019
(This article belongs to the Special Issue Amide Bond Activation)


The addition of amide/sulfonamide bonds to alkynes is not only one of the most important strategies for the direct functionalization of carbon–carbon triple bonds, but also a powerful tool for the downstream transformations of amides/sulfonamides. The present review provides a comprehensive summary of amide/sulfonamide bond addition to alkynes, including direct and metal-free aminoacylation, based-promoted aminoacylation, transition-metal-catalyzed aminoacylation, organocatalytic aminoacylation and transition-metal-catalyzed aminosulfonylation of alkynes up to December 2018. The reaction conditions, regio- and stereoselectivities, and mechanisms are discussed and summarized in detail. View Full-Text
Keywords: amide bond; sulfonamide bond; alkynes; addition reaction; aminoacylation; aminosulfonylation amide bond; sulfonamide bond; alkynes; addition reaction; aminoacylation; aminosulfonylation

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Zhao, F.; Li, P.; Liu, X.; Jia, X.; Wang, J.; Liu, H. Recent Advances in the Addition of Amide/Sulfonamide Bonds to Alkynes. Molecules 2019, 24, 164.

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