Construction of 4-hydroxycoumarin derivatives with adjacent quaternary and tertiary stereocenters ternary catalysis.

4-Hydroxycoumarin derivatives represent one of the most important scaffolds in biologically active substances, pharmaceuticals and functional materials. Herein, we describe an efficient Pd/amine/Brønsted acid ternary-catalytic multicomponent reaction for the rapid construction of substituted 4-hydroxycoumarin derivatives with adjacent quaternary and tertiary stereocenters convergent assembly of two generated active intermediates. Furthermore, the late-stage transformations of coumarin derivatives and their trial of antitumor activity successfully demonstrated the potential utilities of the products as platform molecules.