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Cu-Mediated Expeditious Annulation of Alkyl 3-Aminoacrylates with Aryldiazonium Salts: Access to Alkyl N2-Aryl 1,2,3-Triazole-carboxylates for Druglike Molecular Synthesis

Hao-Nan Liu, Hao-Qiang Cao, Chi Wai Cheung* and Jun-An Ma*

*Department of Chemistry, Tianjin University, Tianjin 300072, P. R. of China, Email:,

H.-N. Liu, H.-Q. Cao, C. W. Cheung, J.-A. Ma, Org. Lett., 2020, 22, 1396-1401.

DOI: 10.1021/acs.orglett.0c00006 (free Supporting Information)

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A Cu-mediated annulation reaction of alkyl 3-aminoacrylates with aryldiazonium salts provides alkyl N2-aryl 1,2,3-triazole-carboxylates rapidly under mild conditions. Furthermore, alkyl 2-aminoacrylates are also viable substrates.

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ID: J54-Y2020