4.8 Article

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

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ORGANIC LETTERS
卷 22, 期 4, 页码 1396-1401

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AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c00006

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  1. National Key Research and Development Program of China [2019YFA0905100]
  2. National Natural Science Foundation of China [21772142, 21971186, 21961142015]
  3. Tianjin University

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Alkyl N-aryl 1,2,3-triazole-carboxylates are important molecules or intermediates in medicinal chemistry, but the synthesis of N-2-aryl counterparts remains elusive. Herein, we describe a Cu-mediated annulation reaction of alkyl 3-aminoacrylates with aryldiazonium salts, both of which are readily available substrates. Furthermore, alkyl 2-aminoacrylates are also viable substrates. Diverse alkyl N-2 -aryl 1,2,3-triazole-carboxylates and their analogues can be rapidly prepared under mild conditions. Especially, this protocol allows one to access several druglike variants of carbonic anhydrase inhibitors and celecoxib.

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