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Description

As one of the most pervasive chemical transformations, methylation plays a central role in biology. The prevalence of methyl groups in approved drugs and the rising demand for deutero-methyl analogs drive our pursuit of new methylating agents for isotopologue synthesis. Partially deuterated methyl groups are rare, and their pharmacological and chemical properties remain largely unexplored. Herein, we report the efficient synthesis of mono- and di-deuterated methylating agents that enable access to methyl isotopologues of small molecules and pharmaceuticals. Dibenzothiophene- and thianthrene-based methylating reagents were synthesized from the corresponding alcohols in good yields. These reagents were fully characterized by single-crystal X-ray diffraction and spectroscopic methods, and applied to a wide range of substrates, including drug molecules, to access methyl isotopologues. The reagents proved to be stable, versatile, and simple to prepare. The synthetic pathways and results of this study will be presented.

Publication Date

4-30-2026

Keywords

Organic Syntheses, Isotopes, Methylation

Efficient Strategy for the Synthesis of

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