Late-stage oxidative C(sp³)-H methylation.

ABSTRACT: Frequently referred to as the 'magic methyl effect', the installation of methyl groups-especially adjacent (α) to heteroatoms-has been shown to dramatically increase the potency of biologically active molecules^1-3. However, existing methylation methods show limited scope and have not been demonstrated in complex settings¹. Here we report a regioselective and chemoselective oxidative C(sp³)-H methylation method that is compatible with late-stage functionalization of drug scaffolds and natural products. This combines a highly site-selective and chemoselective C-H hydroxylation with a mild, functional-group-tolerant methylation. Using a small-molecule manganese catalyst, Mn(CF₃PDP), at low loading (at a substrate/catalyst ratio of 200) affords targe

SUBMITTER: Feng K 

PROVIDER: S-EPMC8006464 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature