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Study on the green click-chemistry synthesis of 4-trifluoroacetyl-1,2,3-triazoles
Authors:Jie Han  Jian-Xiong Ran  Xiu-Ping Chen  Zhong-Hua Wang  Fan-Hong Wu
Institution:1. School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai, China;2. Shanghai Engineering Research Center of Pharmaceutical Progress, Shanghai, 201203, China
Abstract: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.
Keywords:Click-chemistry  Metal-free  Solvent free  Anti-cancer activities
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