Construction of 4-hydroxycoumarin derivatives with adjacent quaternary and tertiary stereocenters via 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/Bronsted acid ternary-catalytic multicomponent reaction for the rapid construction of substituted 4-hydroxycoumarin derivatives with adjacent quaternary and tertiary stereocenters via convergent assembly of two in situ generated active intermediates. Furthermore, the late-stage transformations of coumarin derivatives and their in vitro trial of antitumor activity successfully demonstrated the potential utilities of the products as platform molecules.

Automated summary

This paper describes an efficient ternary-catalytic multicomponent reaction for the rapid construction of 4-hydroxycoumarin derivatives. The potential utilities of the products as platform molecules are demonstrated through late-stage transformations and in vitro trial of antitumor activity.