Recent Advances on Direct Phosphorothiolation Reactions

Abstract Organophosphorothioates are organic molecules containing sulfur and phosphorus, with significant biological activity and physicochemical properties, widely used in organic synthesis, medicinal chemistry, and the agrochemical industry. In particular, many phosphorothioates display a variety of biological activities, such as antifungal, antibacterial, anti‐parasite, anticancer, and so on. Traditionally, the synthesis of phosphorothioates has mainly relied on indirect methods involving the construction of S−P bond. In recent years, direct phosphorothiolation has gained attention as a reliable and rapid method for introducing the −S−P(O)(OR) 2 group into parent molecules. This article reviews the latest advances in direct phosphorothiolation reactions, categorized based on the different sources of the −S−P(O)(OR) 2 group.