Issue 9, 2021

Installing the “magic methyl” – C–H methylation in synthesis

Abstract

The selective and efficient C–H methylation of sp2 and sp3 carbon centres has become a powerful transformation in the synthetic toolbox. Due to the potential for profound changes to physicochemical properties attributed to the installation of a “Magic Methyl” group at a strategic site in a lead compound, such techniques have become highly desirable in modern drug discovery and synthesis programmes. This review will cover the diverse techniques that have been employed to enable the selective installation of the C–Me bond in a wide range of chemical structures, from simple building blocks to complex drug-like architectures.

Graphical abstract: Installing the “magic methyl” – C–H methylation in synthesis

Article information

Article type
Review Article
Submitted
01 Dec 2020
First published
10 Mar 2021
This article is Open Access
Creative Commons BY license

Chem. Soc. Rev., 2021,50, 5517-5563

Installing the “magic methyl” – C–H methylation in synthesis

D. Aynetdinova, M. C. Callens, H. B. Hicks, C. Y. X. Poh, B. D. A. Shennan, A. M. Boyd, Z. H. Lim, J. A. Leitch and D. J. Dixon, Chem. Soc. Rev., 2021, 50, 5517 DOI: 10.1039/D0CS00973C

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