Cu(II)-Mediated Ortho C–H Alkynylation of (Hetero)Arenes with Terminal Alkynes

Ming Shang, Hong-Li Wang, Shang-Zheng Sun, Hui-Xiong Dai, and Jin-Quan Yu

J. Am. Chem. Soc.,
2014, 136, 33, 11590-11593; 10.1021/ja507704b


The Yu group describe an alternative disconnection to the Sonogashira coupling.

Copper(II)-catalyzed ortho alkynylation of arenes and heteroarenseswith terminal alkynes provides an effective entry to aryl alkynes, molecular motifs of huge pharmaceutical significance.

This is part of a continuing program from the Yu group exploring the application of copper-catalysts for C–H functionalization.

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