Journal
SYNLETT
Volume 29, Issue 4, Pages 375-382Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0037-1609093
Keywords
methylation; methyl effect; iodomethane; C-H activation; aryl halides; cross-coupling; nickel catalysis
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Funding
- Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases
- 1000 Talents Recruitment Program
- Tsinghua-Peking Centre for Life Sciences
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Owing to the 'magic methyl effect' on a compound's physical and biological properties, methylation is a strategy frequently used by medicinal chemists in structure-activity relationship studies or in lead optimization. This article highlights the most recent reported methods for the direct methylation of (hetero) arenes, which mainly involve either C-H functionalization or cross-coupling of methylating reagents with (hetero) aryl halides. Methylation of C-H bonds of (hetero)arenes, which is atom economical, has been explored by several research groups in recent years. Given the unmatchable availability of (hetero) aryl halides, we believe that Ni-catalyzed methylation using iodomethane or deuterated iodomethane as the methyl source is one of the most convenient methods.
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