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Recent Progress in Methylation of (Hetero)Arenes by Cross-Coupling or C-H Activation

Hu, Lu, Liu, Yahu and Liao, Xuebin (2018) Recent Progress in Methylation of (Hetero)Arenes by Cross-Coupling or C-H Activation. Synlett, 29 (4). pp. 375-382. ISSN 14372096


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.

Item Type: Article
Keywords: aryl halides C-H activation cross-coupling iodomethane methyl effect methylation nickel catalysis
Date Deposited: 13 Mar 2018 00:45
Last Modified: 25 Jan 2019 00:45


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