Sulfoximines, the monoaza analogues of sulfones featuring a stereogenic sulfur atom,
have emerged as highly versatile molecular frameworks due to their remarkable chemical
stability, tunable electronic properties, and broad applications across pharmaceutical,
agrochemical, and material science domains. The presence of an N(sp²) center imparts
both nucleophilic and basic characteristics, enabling strong coordination with transition
metals and thus expanding their utility in diverse catalytic transformations. Leveraging
this distinctive coordination ability, transition-metal-catalyzed C-H functionalization
directed by sulfoximines has recently gained significant attention as a powerful tool
for the synthesis of complex and value-added molecular architectures. This account
aims to summarize key advancements in the field of stereoselective C-H activation
involving sulfoximines, both as reactive substrates and as chiral directing groups.
Special emphasis is placed on their ability to mediate asymmetric C-H functionalization
processes, where the inherent sulfur centered chirality can be effectively transferred
to neighbouring carbon centers, offering new opportunities for constructing enantioenriched
frameworks with high precision and efficiency.