Issue 4, 2017
From the journal:

Organic Chemistry Frontiers

Metal-free C5-selective halogenation of quinolines under aqueous conditions†

Jichao Chen,a   Tianyu Wang,a   Yanpeng Liu,a   Tong Wang,*ab   Aijun Lin,a   Hequan Yaoa  and  Jinyi Xu*a  

* Corresponding authors

a State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, P. R. China
E-mail: jinyixu@china.com

b Center for Drug Evaluation, China Food and Drug Administration, Beijing 100038, P. R. China
E-mail: wangtong@iccas.ac.cn

Abstract

An efficient and convenient method of C5-selective halogenation of quinoline derivatives was developed. The reaction proceeds smoothly in water with readily available N-halosuccinimides (NCS, NBS and NIS) as the halogenation reagents. This method features metal-free catalysis, no additional oxidants and additives, broad substrate scope and short reaction time.

Graphical abstract: Metal-free C5-selective halogenation of quinolines under aqueous conditions

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Article information

DOI
https://doi.org/10.1039/C6QO00765A
Article type
Research Article
Submitted
29 Nov 2016
Accepted
28 Jan 2017
First published
07 Feb 2017

Org. Chem. Front., 2017,4, 622-626

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Metal-free C5-selective halogenation of quinolines under aqueous conditions

J. Chen, T. Wang, Y. Liu, T. Wang, A. Lin, H. Yao and J. Xu, Org. Chem. Front., 2017, 4, 622 DOI: 10.1039/C6QO00765A

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