Synthesis of Benzopyran-Phenylpropanoid Hybrids via Matsuda-Heck-Arylation and Allylic Oxidation

J Org Chem. 2024 Dec 20;89(24):18585-18601. doi: 10.1021/acs.joc.4c02520. Epub 2024 Dec 7.

Abstract

The synthesis of coumarin- and flavonoid-chalcone hybrids via Pd-catalyzed Heck-type coupling of arene diazonium salts and 8-allylcoumarins and -flavonoids is reported. The β-hydride elimination step proceeds with high regioselectivity if an OMOM-substituent is present at the position C7, adjacent to the allyl group. A selective allylic oxidation of the coupling products was accomplished using DDQ in the presence of silica to furnish the chalcones.