The five-membered oxacyclic system of furan-2(5H)-ones, commonly named as γ-
butenolides or appropriately as Δα,β-butenolides, is of high interest since many studies have proven its
bioactivity. During the past few years, Δα,β-butenolides have been important synthetic targets, with
several reports of new procedures for their construction. A short compendium of the main different
synthetic methodologies focused on the Δα,β-butenolide ring formation, along with selected examples
of compounds with relevant biological activities of these promising pharmaceutical entities is presented.