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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
来源:
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.
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页码:6985 / 6992
页数:8
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