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ACS Omega. 2021 Nov 29;6(49):34044-34055. doi: 10.1021/acsomega.1c05455. eCollection 2021 Dec 14.

Hypervalent Iodine(III)-Promoted C3-H Regioselective Halogenation of 4-Quinolones under Mild Conditions.

ACS omega

Fang Yang, Xiaoqing Wang, Wenzhuo Zhao, Fei Yu, Zhengsen Yu

Affiliations

  1. The Hebei Key Laboratory of Analysis and Control of Zoonotic Pathogenic Micro-organism, College of Life Science, Hebei Agriculture University, Baoding, Hebei 071001, People's Republic of China.
  2. Colleges of Science, Hebei Agriculture University, Baoding, Hebei 071001, People's Republic of China.

PMID: 34926952 PMCID: PMC8675166 DOI: 10.1021/acsomega.1c05455

Abstract

A simple and practical protocol for the C3-H regioselective halogenation of 4-quinolones by the action of potassium halide salt and PIFA/PIDA in good to excellent yields was developed. The current approach provides feasible access to the diversity of C3-halgenated 4-quinolones at room temperature with high regioselectivity and good functional group tolerance, from which bioactive compounds can be easily constructed. Moreover, the current method featured eco-friendly, operational convenience and is suitable for halogenation in a gram scale of 4-quinolones in water without sacrificing yields.

© 2021 The Authors. Published by American Chemical Society.

Conflict of interest statement

The authors declare no competing financial interest.

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