Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 57, Issue 33, Pages 10697-10701Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201804628
Keywords
arenes; C-H activation; cross-coupling; methylation; nickel
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Funding
- Max-Planck-Institut fur Kohlenforschung
- UCB Pharma
- Kwanjeong Educational Foundation
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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.
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