Study on the green click-chemistry synthesis of 4-trifluoroacetyl-1,2,3-triazoles

A metal-free and solvent free click-chemistry procedure has been revealed for the synthesis of 4-trifluoroacetyl-1,2,3-triazoles from corresponding azides and alkyne with high yield and selectivity. The pure products could be easily obtained via crystallization of the reaction mixture (standing for...

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Bibliographic Details
Published in:Tetrahedron 2018-12, Vol.74 (49), p.6985-6992
Main Authors: Han, Jie, Ran, Jian-Xiong, Chen, Xiu-Ping, Wang, Zhong-Hua, Wu, Fan-Hong
Format: Article
Language:English
Subjects:
Anti-cancer activities
Click-chemistry
Metal-free
Solvent free
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Summary:A metal-free and solvent free click-chemistry procedure has been revealed for the synthesis of 4-trifluoroacetyl-1,2,3-triazoles from corresponding azides and alkyne with high yield and selectivity. The pure products could be easily obtained via crystallization of the reaction mixture (standing for 1 day). Among the 4-trifluoroacetyl-1,2,3-triazoles, 3ba showed the best anticancer activity against HepG2 cell with IC50 of 0.0267 μmol/ml. This method has the advantages of less pollution, low cost, simple treatment and more efficiency. [Display omitted]
ISSN:0040-4020
1464-5416
DOI:10.1016/j.tet.2018.10.026