Abstract Enantioselective desymmetrization of prochiral 1,3‐cyclodiketones is the most convenient and highly desired transformation to access densely functionalized, enantiomerically enriched scaffolds with multiple chiral centers. In recent years, organocatalysis has made significant progress in this research area along with other traditional metal‐ or enzyme‐catalyzed reactions. This mini‐review provides an overview of the recent developments in the domain of organocatalytic enantioselective desymmetrization along with a brief discussion about future perspectives.