Journal
ORGANIC LETTERS
Volume 19, Issue 1, Pages 10-13Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b02850
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Funding
- National Natural Science Foundation of China [21572203, J1210042]
- Zhejiang Provincial Natural Science Foundation [LZ16B020001]
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A number of enamine-functionalized 1,2,3-triazole derivatives have been prepared via the Cu-catalyzed three-component reaction of terminal alkyne, azide, and 2H-azirine. The reaction proceeds through insertion of vinyl nitrene into the C-Cu bond of the triazolyl-Cu species, providing an efficient and step- and atom-economic approach to the enamine-bearing polysubstituted 1,2,3-triazoles. The resulting triazoles were easily transformed to trisubstituted pyrazoles in the presence of a Rh catalyst.
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