Department of Chemistry, University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK.
Chem Soc Rev. 2021 May 7;50(9):5517-5563. doi: 10.1039/d0cs00973c. Epub 2021 Mar 10.
The selective and efficient C-H methylation of sp and sp 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.
选择性和高效的 sp 和 sp 碳中心 C-H 甲基化已成为合成工具箱中的一种强大转化。由于在先导化合物的战略位置上安装“神奇甲基”基团可能会导致物理化学性质发生深远变化,因此这些技术在现代药物发现和合成计划中变得非常理想。本综述将涵盖各种技术,这些技术可用于在广泛的化学结构中选择性地安装 C-Me 键,从简单的构建块到复杂的类似药物的结构。