One-Pot Functionalization of 8-Aminoquinolines through the Acylation and Regioselective C5-H Halogenation under Transition-Metal-Free Conditions

被引：7

作者：

Li, Dandan ^{[1
]}

Jia, Zhenzhen ^{[1
]}

Jiang, Yongshuai ^{[1
]}

Jia, Jingpeng ^{[1
]}

Zhao, Xiaowei ^{[1
]}

Li, Zehui ^{[1
]}

Xu, Zhihong ^{[1
]}

机构：

[1] Xuchang Univ, Sch Chem & Chem Engn, 88 Bayi Rd, Xuchang 461000, Henan, Peoples R China

来源：

CHEMISTRYSELECT | 2019年 / 4卷 / 47期

基金：

中国国家自然科学基金;

关键词：

C5-H Halogenation; 8-aminoquinolines; acyl halides; acylation; transition metal free; H BOND FUNCTIONALIZATIONS; N-FLUOROBENZENESULFONIMIDE; C(SP(3))-H BONDS; DIRECTING GROUPS; SODIUM-HALIDES; QUINOLINES; COPPER; IODINATION; ACTIVATION; AMIDES;

D O I：

10.1002/slct.201904286

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A mild and efficient functionalization of 8-aminoquinolines has been demonstrated through the acylation and regioselective C5-H halogenation in one pot under transition metal free conditions. This method enables the acyl halides acting as the donors of both acyl and halide atoms. Moremover, different type of acyl halides could be employed in this reaction and proceeded smoothly to afford the corresponding halogenated products in moderate to good yields. The protocol is operationally simple, facile, and might have potential application in synthesis of 5-halogenated quinoline scaffolds.

引用

页码：13964 / 13967

页数：4

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