Sustainable Stereoselectivity Through Ugi/ Post‐Ugi Modifications: Insights from Recent Literature (2019–2025)

This review focuses on current developments in the asymmetric Ugi four‐component reaction (Ugi‐4CR), emphasizing post‐reaction modifications, catalyst discovery, and stereoselective control. Highly enantioenriched compounds have been synthesized using the combination of chiral and non‐chiral catalysts, such as base‐mediated systems, cobalt, copper, and palladium. Additionally, Ugi‐derived molecules are now more applicable in material science, peptide synthesis, and drug discovery due to post‐Ugi modifications such as cyclization and cross‐coupling processes. Emphasizing the relevance of asymmetric Ugi‐4CR in contemporary sustainable chemical synthesis, the discussion focuses on mechanistic insights, catalytic methods, and emerging applications. The goal of future research is to increase the usefulness of Ugi‐4CR in synthetic and medicinal chemistry by expanding the range of asymmetric transformations and improving catalytic strategies.