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One‐Pot Functionalization of 8‐Aminoquinolines through the Acylation and Regioselective C5‐H Halogenation under Transition‐Metal‐Free Conditions
Author(s) -
Li Dandan,
Jia Zhenzhen,
Jiang Yongshuai,
Jia Jingpeng,
Zhao Xiaowei,
Li Zehui,
Xu Zhihong
Publication year - 2019
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201904286
Subject(s) - regioselectivity , acylation , halogenation , halide , surface modification , chemistry , quinoline , combinatorial chemistry , transition metal , organic chemistry , catalysis
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.