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Rapid and Efficient Pd-Catalyzed Sonogashira Coupling of Aryl Chlorides

He Huang, Hong Liu*, Hualiang Jiang and Kaixian Chen

*Drug Discovery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, and Graduate School, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China, Email:

H. Huang, H. Liu, H. Jiang, K. Chen, J. Org. Chem., 2008, 73, 6037-6040.

DOI: 10.1021/jo800994f (free Supporting Information)

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An efficient and effective microwave-assisted cross-coupling of terminal alkynes with various aryl chlorides including sterically hindered substrates proceeds fast and generally gives coupled products in very good yields. The conditions were extended successfully to Suzuki coupling, Buchwald-Hartwig amination, and the Heck coupling of aryl chlorides.

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Key Words

Sonogashira Coupling, Microwave Synthesis

ID: J42-Y2008-2180