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Updated: Jul 11, 2025

Efficient Synthesis of All-Carbon Quaternary Centers via the Conjugate Addition of Functionalized Monoorganozinc Bromides
Published on: May 26, 2019
Construction of 4-hydroxycoumarin derivatives with adjacent quaternary and tertiary stereocenters via ternary
Mengchu Zhang1, Tianyuan Zhang1, Sifan Yu1
1School of Pharmaceutical Sciences, Sun Yat-sen University Guangzhou 510006 China qianyu5@mail.sysu.edu.cn huwh9@mail.sysu.edu.cn.
Abstract:
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 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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