Abstract:R-Glabridin is one of the unique isoflavones in glycyrrhiza glabra, which has a broad spectrum of biological activities. In this study, R-glabridin has been obtained via seven steps from 7-hydroxychromen-4-one by protection of phenolic hydroxyl groups, esterification of enol, Heck asymmetric coupling, deprotection, cyclization, reduction and demethylation and so on, the total yield was 23.5% and the ee value of the final product was 98.9%. The structures of products were confirmed by 1HNMR and MS. This method has the advantage of mild reaction conditions, easy operation and high yield.