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Cu/Pd-Catalyzed, Three-Component Click Reaction of Azide, Alkyne, and Aryl Halide: One-Pot Strategy toward Trisubstituted Triazoles

Fang Wei, Haoyu Li, Chuanling Song, Yudao Ma, Ling Zhou, Chen-Ho Tung and Zhenghu Xu*

*Key Lab for Colloid and Interface Chemistry of Education Ministry, School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, China, Email:

F. Wei, H. Li, C. Song, Y. Ma, L. Zhou, C.-H. Tung, Z. Xu, Org. Lett., 2015, 17, 2860-2863.

DOI: 10.1021/acs.orglett.5b01342

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A Cu/Pd transmetalation relay catalysis enables a three-component click reaction of azide, alkyne, and aryl halide to yield 1,4,5-trisubstituted 1,2,3-triazoles in one step in high yields with complete regioselectivity. This reaction offers an alternative to the well-established CuAAC click reactions only working on terminal alkynes.

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Key Words

1,2,3-triazoles, multicomponent reactions

ID: J54-Y2015