Chiral Isothiourea-Catalyzed Acylative Dynamic Kinetic Resolu-tion of 3-Hydroxyphthalides for Enantioselective Synthesis of Phthalidyl Ester

Phthalides serve as core structures pervasive in a wide array of natural products and drug molecules, which display a diverse array of biological activities. We report herein a highly efficient dynamic kinetic resolution of 3-hydroxyphthalides by chiral isothioureas (ITUs) catalyzed asymmetric acylation, facilitating the effective synthesis of a variety of chiral phthalidyl esters with good yields and enanti-oselectivities. Notably, this reaction features mild reaction conditions, expansive substrate scope as well as good functional group compatibility. In addition, the practicality of this method is underscored by the large-scale synthesis, reduced catalyst loading exper-iment and the synthesis of the chiral phthalidyl ester prodrug.