Selective Methylation of Arenes: A Radical C-H Functionalization/Cross-Coupling Sequence.
Fabien SerpierFei PanWon Seok HamJérôme JacqChristophe GenicotTobias RitterPublished in: Angewandte Chemie (International ed. in English) (2018)
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.