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Chinese Journal of Organic Chemistry >

0 3001

DOI: https://doi.org/10.6023/cjoc202603001

REVIEW

Research Progress on the Construction of Optically Pure α-Keto Monofluoro Chiral Centers

  • Jin Cheng ,
  • Zhu Xin ,
  • Wu Xianyao ,
  • Wu Fulong ,
  • Wang Changjuan ,
  • Lian Xiang ,
  • Wu Jingjing ,
  • Wu Fanhong
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  • aFaculty of Chemical Engineering and Energy Technology, Shanghai Institute of Technology, Shanghai 201418
    bShanghai Engineering Research Center of Green Fluoropharmaceutical Technology, Shanghai 201418
    cZhejiang Hissen Pharmaceutical Co., Ltd., Dongyang, Zhejiang 322100

Received date: 2026-03-02

  Revised date: 2026-05-11

  Online published: 2026-06-18

Supported by

National Natural Science Foundation of China (No. 22403066, 21672151 and 21602136).

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Abstract

Fluorinated organic compounds, endowed with unique physicochemical properties, have found extensive applications in pivotal fields including pharmaceuticals, agrochemicals, and materials science. Notably, enantiomerically pure α-carbonyl monofluorinated compounds containing chiral centers have garnered considerable attention in drug discovery in recent years, owing to their crucial role in regulating biological activity and modulating molecular configuration. This review systematically summarizes the major synthetic strategies for constructing such structures over the past decade, which are categorized into three aspects: (1) Achievement of asymmetric fluorination through C—F bond formation; (2) Asymmetric formation of C—C bonds utilizing fluorinated nucleophilic or electrophilic building blocks; (3) Emerging radical and synergistic catalysis modes. By critically analyzing the electronic and steric effects of fluorine atoms on reaction activity and stereoselectivity, we assess the substrate scope and inherent limitations of existing methodologies, aiming to provide rational design principles for the future synthesis of monofluorinated chiral centers.

Key words： α-fluoroketone; chiral center; asymmetric fluorination; fluorine-containing building

Cite this article

Jin Cheng , Zhu Xin , Wu Xianyao , Wu Fulong , Wang Changjuan , Lian Xiang , Wu Jingjing , Wu Fanhong . Research Progress on the Construction of Optically Pure α-Keto Monofluoro Chiral Centers[J]. Chinese Journal of Organic Chemistry, 0 : 3001 . DOI: 10.6023/cjoc202603001

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