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Molecules 2012, 17(1), 240-247; https://doi.org/10.3390/molecules17010240

Practical Synthesis of Hydroxychromenes and Evaluation of Their Biological Activity

1
Institute of Life Science Research, Rexgene Biotech, Ochang, Chungbuk 363-838, Korea
2
Department of Neuroscience and TIDRC, School of Medicine, Ewha Womans University, Seoul 158-710, Korea
*
Author to whom correspondence should be addressed.
Received: 5 December 2011 / Revised: 24 December 2011 / Accepted: 26 December 2011 / Published: 28 December 2011
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Abstract

A simple and efficient seven steps synthesis of brodifacoum and difethialone from phenylacetyl chloride is described. The key synthetic strategies involve Friedel-Crafts acylation, intramolecular ring cyclization and condensation reaction in the presence of Brønsted-Lowry acids. It was found that brodifacoum showed favorable inhibiting activities on LPS-stimulated nitrite production in BV-2 microglia cells. Brodifacoum exhibited superior anti-inflammatory effects than difethialone. We expect that an efficient linear synthesis of 4-hydroxycoumarin derivatives and key fragments that are useful agents for the modulation of inflammation as well as inhibition of coagulation will be of practical use. View Full-Text
Keywords: anti-inflammatory; brodifacoum; coupling reaction; difethialone; Friedel-Crafts acylation; intramolecular ring cyclization reaction anti-inflammatory; brodifacoum; coupling reaction; difethialone; Friedel-Crafts acylation; intramolecular ring cyclization reaction
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Jung, J.-C.; Oh, S. Practical Synthesis of Hydroxychromenes and Evaluation of Their Biological Activity. Molecules 2012, 17, 240-247.

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