Recent Advances in the Synthesis and <i>N</i> ‐Functionalization of Sulfonimidamides

Abstract Sulfonimidamides (SIAs) have garnered broad interests from medicinal chemists owing to their diverse and broad spectrum biological activities. This class of organosulfur compounds has also demonstrated promising applications in agriculture and materials science. In order to obtain structurally diverse SIAs and their N ‐functionalized derivatives, a variety of synthetic methodologies have been developed. This review highlights the key discoveries and recent advances in this dynamic and rapidly evolving research field over the past decade. The synthetic approaches for SIAs include conventional synthetic methods, photocatalytic synthesis, transition metal‐catalyzed reactions, mechanochemical strategies, and SuFEx chemistry. Meanwhile, the N ‐functionalization reactions encompass N‐ aliphatic alkylation, N ‐acylation, N ‐arylation, and N ‐sulfenylation. The challenges of N ‐functionalization and outlooks on the application of SIAs are also concluded in this review.