期刊
ORGANIC LETTERS
卷 22, 期 4, 页码 1396-1401出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c00006
关键词
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资金
- National Key Research and Development Program of China [2019YFA0905100]
- National Natural Science Foundation of China [21772142, 21971186, 21961142015]
- Tianjin University
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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