Synthesis 2025; 57(19): 2753-2764
DOI: 10.1055/a-2616-5364
Short Review

Recent Developments of Monofluorination via Three-Component Reactions

Autoren

  • Fumin Shen

    1   School of Pharmacy, Xinxiang University, Xinxiang, PR China
  • Jingjing Yao

    1   School of Pharmacy, Xinxiang University, Xinxiang, PR China
  • Siying Xu

    1   School of Pharmacy, Xinxiang University, Xinxiang, PR China
  • Ran Xia

    1   School of Pharmacy, Xinxiang University, Xinxiang, PR China
  • Zhan-Yong Wang

    1   School of Pharmacy, Xinxiang University, Xinxiang, PR China

Funding information Funded by The Natural Science Foundation of Henan Province 232300420142.


Graphical Abstract

Abstract

The incorporation of fluorine into organic molecules holds significant value. The three-component reaction provides a more convenient approach for the synthesis of organofluorine compounds. Radical monofluorination will be fully discussed in this review. Besides, other methods like transition metal-catalyzed, electrophilic, nucleophilic, and carbine-mediated conditions will also be discussed. There are two main methods for producing monofluorinated compounds: forming C–F bonds using fluorinating agents or creating C–C bonds with fluorinated substrates. The latter method boasts a wider range of applicable substrates. We will discuss reactions involving various substrates, including NFSI, KHF2, Selectfluor, FABI, Et3N·3HF, COF2, ICH2F, DAST, and others. We will review the advancements made over the past decade (2014–2024) and offer explanations of the underlying mechanisms. Additionally, how the additive reagents work will also be discussed.



Publikationsverlauf

Eingereicht: 10. April 2025

Angenommen nach Revision: 20. Mai 2025

Accepted Manuscript online:
20. Mai 2025

Artikel online veröffentlicht:
07. August 2025

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