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Journal Article

Selective Methylation of Arenes: A Radical C−H Functionalization/Cross‐Coupling Sequence

MPS-Authors
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Serpier,  Fabien
Research Department Ritter, Max-Planck-Institut für Kohlenforschung, Max Planck Society;

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Pan,  Fei
Research Department Ritter, Max-Planck-Institut für Kohlenforschung, Max Planck Society;

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Ham,  Won-Seok
Research Department Ritter, Max-Planck-Institut für Kohlenforschung, Max Planck Society;
Department of Chemistry and Chemical Biology, Harvard University;

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Ritter,  Tobias
Research Department Ritter, Max-Planck-Institut für Kohlenforschung, Max Planck Society;
Department of Chemistry and Chemical Biology, Harvard University;

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(Supplementary material), 11MB

Citation

Serpier, F., Pan, F., Ham, W.-S., Jacq, J., Genicot, C., & Ritter, T. (2018). Selective Methylation of Arenes: A Radical C−H Functionalization/Cross‐Coupling Sequence. Angewandte Chemie International Edition, 57(33), 10697-10701. doi:10.1002/anie.201804628.


Cite as: https://hdl.handle.net/21.11116/0000-0001-E5E9-6
Abstract
A selective, nonchelation‐assisted methylation of arenes has been developed. The overall transformation, which combines a C−H functionalization reaction with a nickel‐catalyzed cross‐coupling, offers rapid access to methylated arenes with high para selectivity. The reaction is amenable to late‐stage methylation of small‐molecule pharmaceuticals.