Recent Progress in the Synthesis of Sulfonylmethyl Compounds Using Diverse Sulfonylmethylating Reagents

Sulfonylmethyl motif is widely present in many organic compounds and has shown important application in pharmaceutical chemistry, organic synthesis, and materials science. In recent years, considerable attention has been devoted to the development of efficient methods for constructing sulfonylmethyl‐containing compounds. This review focuses on summarizing the research progress from 2010 to 2025 in the synthesis of sulfonylmethyl compounds via various sulfonylmethylating reagents, including methylarylsulfones, halogenated methyl sulfones, and sulfonylmethyl isocyanide, as well as the coupling of C1 synthons with sulfone sources. Representative reaction modes and related mechanistic aspects are also discussed. This review aims to provide a systematic overview and useful reference for the further development and application of sulfonylmethylation chemistry.