Asymmetric desymmetrization: Simultaneous stereocontrol of multichiral centers

Asymmetric desymmetrization is an efficient and powerful methodology for optically active substances with complex structures. Enantiotopic group differentiation reactions starting from meso compound with chiral centers can afford chiral/non-racemic compounds bearing controlled multi-chiral centers. We introduce many useful examples of asymmetric desymmetrization, which have ever been reported, and our results on asymmetric desymmetrization using asymmetric ene reactions catalyzed by chiral BINOL-Ti complex.