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August 6, 2026Beilstein Journal of Organic ChemistryOpen Access

Construction of CF 2 moieties in FDA-approved drugs (2016–2025): industrial routes, mechanisms, and scale-up considerations

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Authors

WYWenyan YaoHZHuanhuan ZhangXYXiaolong Yang

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Overview

Review examines synthetic processes for CF2-containing drugs, highlighting industrial routes and mechanisms.

Key Points

  • This review analyzes the construction of CF2 moieties in FDA-approved drugs from 2016 to 2025, focusing on synthetic methods and industrial applicability.
  • Systematic examination of 12 FDA-approved CF2-containing drugs from 2016 to 2025.
  • Classification of CF2 formation methods into fluorinating reagent-based and building block-based approaches.
  • Discussion of four reaction mechanisms: nucleophilic fluorination, electrophilic fluorination, radical pathways, and carbene insertion.
  • Industry favors preformed CF2 building blocks or indirect fluorination strategies for alkyl-CF2 groups to avoid hazardous reagents.
  • Metal-catalyzed techniques for heteroaryl-CF2 still face industrial challenges.
  • The difluorocarbene route for ArO-CF2 has been validated for industrial application.

Cite This Study

Yao et al. (2026) studied this question.

synapsesocial.com/papers/6a7437d4764cddc9499d58eehttps://doi.org/10.3762/bjoc.22.91
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