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

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.

SUBMITTER: Yang F

PROVIDER: S-EPMC8675166 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature

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

Yang Fang F Wang Xiaoqing X Zhao Wenzhuo W Yu Fei F Yu Zhengsen Z

ACS omega 20211129 49

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 ...[more]

PMID: 34926952

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