Catalytic C–H Functionalization Methods Open access Peer reviewed

Versatile Cobalt(III)-Catalyzed Chemoselective C−H Alkylation with Polyfunctional Alkylzinc Reagents

Tsuyoshi Oyama, Stig D. Friis, Elisa Lai, Magnus J. Johansson and 1 more

ACS Catalysis | Jun 1, 2026

Abstract

Abstract

C(sp2)−C(sp3) bond-forming reactions, which can increase the Fsp3 carbons, have emerged as a valuable approach for drug discovery. Herein, we report on the cobalt(III)-catalyzed chemoselective C(sp2)−H alkylation using bifunctional alkylzinc reagents as alkylation agents. The mild nucleophilic nature of organozinc reagents and the mild reaction conditions translated into a broad functional group tolerance and thus enabled the late-stage functionalization of highly functionalized drug molecules. In addition, the use of an earth-abundant cobalt catalyst and low-toxic zinc reagents highlighted an environmentally benign system.

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Tsuyoshi Oyama

first | University of Göttingen | ORCID 0009-0008-3434-6612

Stig D. Friis

middle | AstraZeneca (Australia) | ORCID 0000-0003-4330-5173

Elisa Lai

middle | AstraZeneca (Australia)

Magnus J. Johansson

middle | AstraZeneca (Australia) | ORCID 0000-0002-0904-2835

Prof. Dr. Lutz Ackermann

last | University of Göttingen

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Citation

BibTeX

@article{Oyama2026Versatile,
  title = {Versatile Cobalt(III)-Catalyzed Chemoselective C−H Alkylation with Polyfunctional Alkylzinc Reagents},
  author = {Tsuyoshi Oyama and Stig D. Friis and Elisa Lai and Magnus J. Johansson and Prof. Dr. Lutz Ackermann},
  journal = {ACS Catalysis},
  year = {2026},
  doi = {10.1021/acscatal.6c02833},
  url = {https://doi.org/10.1021/acscatal.6c02833}
}

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