Amine‐Ligated Boryl Radicals Enables Direct C─F Borylation and Cross‐Couplings of Polyfluoroarenes
Polyfluoroarenes are privileged scaffolds in pharmaceutical and materials science, yet their synthesis remains challenging. Aromatic borylation offers a modular entry point for derivatization via Suzuki-Miyaura cross-coupling, but progress is hindered by two persistent issues: the difficulty of direct borylation on electron-deficient polyfluoroarenes, and the pronounced susceptibility of the resulting boron species to rapid protodeboronation under standard cross-coupling conditions. Here, we present an orthogonal strategy that addresses both limitations. Amine-ligated boryl radicals enable direct radical C─F borylation of polyfluoroarenes under visible-light photoredox catalysis. The resulting amine-borane adducts are crystalline, bench-stable, and resistant to protodeboronation, allowing their direct use in Pd-catalyzed Suzuki-Miyaura cross-couplings. This platform provides scalable and broadly applicable access to functionalized polyfluoroarenes and overcomes some of the synthetic constraints associated with these valuable motifs.
Authors
- Tsunayoshi Takehara (ORCID: https://orcid.org/0000-0002-4113-7578)
- Shuichi Nakamura (ORCID: https://orcid.org/0000-0001-5633-8367)
- Daniele Leonori (ORCID: https://orcid.org/0000-0002-7692-4504)
- Naoki Yasukawa (ORCID: https://orcid.org/0000-0002-7994-0470)
- Ryota Nomura (ORCID: https://orcid.org/0000-0001-5510-8535)
- Takeyuki Suzuki (ORCID: https://orcid.org/0000-0002-2137-0276)
- Ryota Kawamura
- Waka Okada
- Marc Fimm
Institutions
- Nagoya Institute of Technology (JP)
- Osaka Research Institute of Industrial Science and Technology (JP)
- RWTH Aachen University (DE)
- The University of Osaka (JP)
Publication Details
- Journal
- Angewandte Chemie International Edition
- Published
- 2025-09-23
- DOI
- https://doi.org/10.1002/anie.202514741
- Citations
- 3
- Primary Topic
- Radical Photochemical Reactions
- Type
- article
- Field-Weighted Citation Impact
- 2.81
Funders
- Takahashi Industrial and Economic Research Foundation
- Japan Society for the Promotion of Science