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

被引:8
|
作者
Han, Jie [1 ]
Ran, Jian-Xiong [1 ]
Chen, Xiu-Ping [1 ]
Wang, Zhong-Hua [1 ,2 ]
Wu, Fan-Hong [1 ]
机构
[1] Shanghai Inst Technol, Sch Chem & Environm Engn, Shanghai, Peoples R China
[2] Shanghai Engn Res Ctr Pharmaceut Progress, Shanghai 201203, Peoples R China
基金
中国国家自然科学基金;
关键词
Click-chemistry; Metal-free; Solvent free; Anti-cancer activities; 1,3-DIPOLAR CYCLOADDITION; REACTION METRICS; AZIDE; ROUTE; REGIOSELECTIVITY; 1,2,3-TRIAZOLES; DERIVATIVES; ANTICANCER; IMPACT;
D O I
10.1016/j.tet.2018.10.026
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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 mu mol/ml. This method has the advantages of less pollution, low cost, simple treatment and more efficiency. (C) 2018 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6985 / 6992
页数:8
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