Copper(I) and N-fluorobenzenesulfonimide-mediated direct regioselective halogenation of 8-amidoquinolines on the C5 position

被引:37
作者
He, Xin [1 ,2 ]
Xu, Yi-zhu [1 ]
Kong, Ling-xuan [3 ]
Wu, Huan-huan [1 ]
Ji, De-zhong [1 ,3 ]
Wang, Zhi-bin [3 ]
Xu, Yun-gen [1 ,3 ]
Zhu, Qi-hua [1 ,3 ]
机构
[1] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
[2] Changzhou Vocat Inst Engn, Changzhou 213164, Peoples R China
[3] China Pharmaceut Univ, Dept Med Chem, Jiangsu Key Lab Drug Design & Optimizat, Nanjing 210009, Jiangsu, Peoples R China
来源
ORGANIC CHEMISTRY FRONTIERS | 2017年 / 4卷 / 06期
关键词
MILD CONDITIONS; H ACTIVATION; DIRECT ARYLATION; C-8; POSITION; LIVING CELLS; QUINOLINES; OXIDES; FUNCTIONALIZATION; HETEROCYCLES; BONDS;
D O I
10.1039/c6qo00644b
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
An efficient and convenient method for the direct regioselective halogenation of 8-amidoquinolines has been developed. In the presence of CuX and N-fluorobenzenesulfonimide (NFSI), the C5-halogenation products of 8-acylaminoquinolines were obtained in moderate to excellent yields. This new procedure provides facile access to a variety of C5-halogenation of 8-amidoquinolines under mild conditions.
引用
收藏
页码:1046 / 1050
页数:5
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