Constructing stereogenic sulfur(vi) centers by catalytic desymmetrization: strategies and prospects

Abstract

Sulfur-stereogenic S(VI) motifs are key structural elements in pharmaceuticals and bioactive compounds. Catalytic desymmetrization of prochiral sulfoximines and sulfonimidamides has emerged as a versatile strategy, circumventing the inefficiencies of traditional resolution or chiral pool approaches. Beyond metal-catalyzed C–H activation, organocatalysis and palladium-catalyzed C–N coupling have proven powerful complements, enabling stereocontrol via hydrogen-bonding, ion-pairing, or chiral ligand design. This review summarizes the latest advancements in catalytic desymmetrization, highlighting its power and generality in the formation of stereogenic sulfur(VI) centers.