Late-Stage C(sp³)-H Methylation of Drug Molecules.

ABSTRACT: Methyl groups are well understood to play a critical role in pharmaceutical molecules, especially those bearing saturated heterocyclic cores. Accordingly, methods that install methyl groups onto complex molecules are highly coveted. Late-stage C-H functionalization is a particularly attractive approach, allowing chemists to bypass lengthy syntheses and facilitating the expedited synthesis of drug analogues. Herein, we disclose the direct introduction of methyl groups via C(sp³)-H functionalization of a broad array of saturated heterocycles, enabled by the merger of decatungstate photocatalysis and a unique nickel-mediated S_H2 bond formation. To further demonstrate its synthetic utility as a tool for late-stage functionalization, this method was applied t

SUBMITTER: Mao E 

PROVIDER: S-EPMC10680140 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature