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Metal-Free Synthesis of 2-Fluoroalkylated Quinolines Using Polyfluoroalkanoic Acids as Direct Fluorine Sources
被引:33
|作者:
Nan, Jiang
[1
]
Hu, Yan
[1
]
Chen, Pu
[1
]
Ma, Yangmin
[1
]
机构:
[1] Shaanxi Univ Sci & Technol, Coll Chem & Chem Engn, Shaanxi Key Lab Chem Addit Ind, Xian 710021, Shaanxi, Peoples R China
基金:
中国博士后科学基金;
关键词:
ONE-POT SYNTHESIS;
TRIFLUOROACETIC-ACID;
3-COMPONENT SYNTHESIS;
FACILE SYNTHESIS;
TRIFLUOROMETHYLATION;
CYCLIZATION;
CHLORIDES;
ARYL;
DIFLUOROMETHYLATION;
BROMIDES;
D O I:
10.1021/acs.orglett.9b00039
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
A novel [5 + 1] cyclization of 2-vinylanilines with polyfluoroalkanoic acids under catalyst- and additive-free conditions was successfully implemented. The approach directly employs very low-cost and readily available polyfluoroalkanoic acids as both Cl synthons and fluoroalkyl building blocks. This method provides concise access to diverse 2-fluoroalkylated (CF3, C2F5, C3F2, CF2H, CF2Cl, and CF2Br) quinolines in good yields with excellent functional group tolerance in high yield on a gram scale.
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页码:1984 / 1988
页数:5
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