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.

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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

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article

Amine‐Ligated Boryl Radicals Enables Direct C─F Borylation and Cross‐Couplings of Polyfluoroarenes

Tsunayoshi Takehara, Shuichi Nakamura, Daniele Leonori, Naoki Yasukawa et al.
3 citations
Angewandte Chemie International Edition
Radical Photochemical Reactions
2.81
article

Amine‐Ligated Boryl Radicals Enables Direct C─F Borylation and Cross‐Couplings of Polyfluoroarenes

Tsunayoshi Takehara, Shuichi Nakamura, Daniele Leonori, Naoki Yasukawa, Ryota Nomura, Takeyuki Suzuki, Ryota Kawamura, Waka Okada, Marc Fimm
article en
3 citations

Abstract

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.

Angewandte Chemie International EditionVol. 64(46)
Nagoya Institute of Technology (JP), Osaka Research Institute of Industrial Science and Technology (JP), RWTH Aachen University (DE), The University of Osaka (JP)
Takahashi Industrial and Economic Research Foundation, Japan Society for the Promotion of Science
Openalex Percentile: Top 9%
Radical Photochemical Reactions
2.81
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