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Synthesis
DOI: 10.1055/a-2616-5364
DOI: 10.1055/a-2616-5364
Short Review
Recent Developments of Monofluorination via Three-Component Reactions
Funding information Funded by The Natural Science Foundation of Henan Province 232300420142.
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.
Publication History
Received: 10 April 2025
Accepted after revision: 20 May 2025
Accepted Manuscript online:
20 May 2025
Article published online:
07 August 2025
© 2025. Thieme. All rights reserved.
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