Late-stage diversification of 5-hydroxyflavones by Suzuki-Miyaura and Buchwald-Hartwig cross-coupling.

Authors

N Delporte, O Cadoret, T Zurbach, D Vijayakumar, P Chalard, J M Lobaccaro, I Abrunhosa-Thomas

Published in

Organic & biomolecular chemistry. Oct 27, 2026. Epub Oct 27, 2026.

Abstract

Late-stage diversification of 5-hydroxyflavones for structure-activity relationship studies was achieved using two classical palladium-catalysed methodologies: Suzuki-Miyaura and Buchwald-Hartwig cross-coupling reactions. Both protocols start from common halogenated 5-hydroxy-3'-trifluoromethylflavone precursors, obtained on a 10 g scale in good overall yield through an optimised Baker-Venkataraman route. Sixteen biaryl flavones were then prepared by conventional heating (41 to 93% yield) and thirteen diarylamino flavones were obtained under microwave irradiation (23 to 99% yield), offering a practical platform for medicinal chemistry applications.

PMID:
42935349
Bibliographic data and abstract were imported from PubMed on 27 Oct 2026.

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