KCS

Asymmetric domino multicatalysis has been emerging as a highly efficient and powerful method for the synthesis of structurally complex molecules from relatively simple starting materials. Recently, we developed a highly efficient NHC-catalyzed domino oxidation/oxa-Michael addition reaction of o-alkenylbenzaldehydes that enabled the easy preparation of a diverse array of 3-substituted phthalides. Chiral 3-substituted phthalides are important classes of naturally occurring lactones that have been found to exhibit a wide range of biological indications and to be versatile building blocks for the synthesis of bioactive compounds. In light of our recent success in NHC-catalyzed domino oxidation/oxa-Michael addition reaction of o-alkenylbenzaldehydes, we investigated a dual catalytic system consisting of an achiral NHC and chiral bifunctional cinchonine for the synthesis of chiral 3-subtituted phthalides.