Issue 44, 2023

Direct synthesis of alkylated 4-hydroxycoumarin derivatives via a cascade Cu-catalyzed dehydrogenation/conjugate addition sequence

Abstract

An efficient approach for the direct synthesis of alkylated 4-hydroxycoumarin derivatives via a Cu-catalyzed cascade dehydrogenation/conjugate addition sequence starting from simple saturated ketones and 4-hydroxycoumarins has been developed. This protocol features excellent functional-group tolerance, easy scale-up, and a broad substrate scope including bioactive molecules. More importantly, a series of marketed drugs, such as warfarin, acenocoumarol, coumachlor, and coumafuryl, can be obtained by this method.

Graphical abstract: Direct synthesis of alkylated 4-hydroxycoumarin derivatives via a cascade Cu-catalyzed dehydrogenation/conjugate addition sequence

Supplementary files

Article information

Article type
Communication
Submitted
22 Apr 2023
Accepted
05 May 2023
First published
06 May 2023

Chem. Commun., 2023,59, 6686-6689

Direct synthesis of alkylated 4-hydroxycoumarin derivatives via a cascade Cu-catalyzed dehydrogenation/conjugate addition sequence

Z. Chen, H. Li, Y. Liao, M. Wang and W. Su, Chem. Commun., 2023, 59, 6686 DOI: 10.1039/D3CC01960H

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