Recent Advances in the Synthesis of Trideuteromethyl Sulfide

Abstract The methylthio group plays a significant role in antitumor bioactive molecules, candidate drugs and natural products. Deuteration modification of drugs, which could prolong the half‐life, reduce toxicity, and enhance targeting, has become an important strategy in the development and discovery of innovative drugs. Combining the unique properties of the methylthio group with the deuteration effect, the rapid introduction of trideuteromethylthiol groups into small organic molecules is essential for advancing the research and development of deuterated drugs. With the rapid development of new trideuteromethylthiolation reagents, this review first outlines the indirect introduction of trideuteromethylthiol groups, and then discusses the direct nucleophilic, electrophilic and free radical trideuteromethylthiolation methods.