Journal
CHEMICAL SCIENCE
Volume 14, Issue 42, Pages 11850-11857Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d3sc03452f
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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.
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.
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