An Update on Total Synthesis and Structural Modifications of Glabridin

Natural products continue to play a pivotal role in medicinal chemistry due to their remarkable structural diversity and wide‐ranging pharmacological activities. Licorice, a well‐known traditional Chinese medicinal herb, is a rich source of bioactive compounds. Among these, glabridin, a prenylated isoflavonoid isolated from licorice root, has attracted considerable attention owing to its diverse biological properties. Total synthesis serves as a critical platform for advancing organic chemistry by enabling the construction of structurally complex natural products from simple starting materials. Over the years, several multistep synthetic strategies have been developed for the preparation of glabridin, commonly originating from simple phenol/resorcinol or coumarin derivatives. These approaches typically involve key transformations such as condensation, cyclization, and reduction to construct the isoflavanone framework. This review provides a comprehensive overview of reported synthetic methodologies for glabridin, with particular emphasis on both racemic and enantioselective approaches. Overall, it summarizes literature reports and patents related to the total synthesis and derivatization of glabridin, which may be useful for synthetic chemists to develop better and more robust synthetic method for glabridin.