Installation of d3-methyl group to drugs by continuous-flow solid-phase synthesis.

ABSTRACT: The d3-methyl group, which combines the "magic methyl effect" and the deuterium effect, is highly sought after by medicinal chemists, resulting in the development of various d3-methyl reagents derived from low-cost, readily available CD₃OD. However, a universally applicable, cost-effective, easily accessible and handleable, highly active, and recyclable d3-methyl reagent remains elusive. Herein, we design a thianthrene-based organic polymer (TT-OP) that shows the ability of capturing and releasing the d3-methyl reagent. This polymer demonstrates excellent loading capacity, scalability, and stability. Utilizing this developed heterogeneous d3-methyl reagent (TT-OP-CD₃), we achieve selective d3-methylation of over 35 biologically active molecules d3-at oxygen, nitrogen,

SUBMITTER: Ou W 

PROVIDER: S-EPMC12663303 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature