Design, Synthesis and Application of a Robust d₃‐Methylthiolating Reagent^†

Abstract

Comprehensive SummaryA deuterated methylthiolating reagent with a broad spectrum, designated as DMTP, has been ingeniously formulated. This new reagent can be produced with high efficiency through the simple combination of commercially available methyl 3‐thiopropanoate and CD3I. This novel SCD3 reagent exhibits excellent reactivity with electrophiles such as alkyl iodides, benzyl chlorides, aryl halides (I, Br) and aryl triflates, resulting in high levels of deuterium content (99% D). Representative deuterated methylthiolated biomolecules, such as Sulfoxaflor, have been synthesized for use in pharmaceutical discovery and development.This article is protected by copyright. All rights reserved.