Recent Advances in the Organocatalytic Enantioselective Synthesis of Functionalized β‐Lactones

This Focus Review highlights recent developments in the organocatalytic enantioselective synthesis of β‐lactone derivatives. Owing to the importance of β‐lactones as a heterocyclic motif that is present in a variety of natural products and biologically active molecules, several catalytic methods have been developed for the synthesis of these compounds in their enantiomerically pure form. Organocatalytic methods that employ N‐heterocyclic carbenes (NHCs), cinchona alkaloids, isothioureas, 4‐dimethylaminopyridine (DMAP) derivatives, and phosphines have allowed the highly enantioselective synthesis of β‐lactones from cheap and readily available starting materials. Moreover, the inherent strain in the four‐membered ring of β‐lactones has also been utilized in further synthetic transformations, thus making β‐lactones a versatile intermediate in organic synthesis. Setting the lac‐tone: A range of organocatalytic methods, including the use of N‐heterocyclic carbenes (NHCs), cinchona alkaloids, isothioureas, 4‐dimethylaminopyridine (DMAP) derivatives, and phosphines, have been used for the highly enantioselective synthesis of β‐lactone derivatives from cheap and readily available starting materials. This Focus Review provides a concise account of recent developments in this field.