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Practical Synthesis of Hydroxychromenes and Evaluation of Their Biological Activity

by 1 and 2,*
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.
Molecules 2012, 17(1), 240-247; https://doi.org/10.3390/molecules17010240
Received: 5 December 2011 / Revised: 24 December 2011 / Accepted: 26 December 2011 / Published: 28 December 2011
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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MDPI and ACS Style

Jung, J.-C.; Oh, S. Practical Synthesis of Hydroxychromenes and Evaluation of Their Biological Activity. Molecules 2012, 17, 240-247. https://doi.org/10.3390/molecules17010240

AMA Style

Jung J-C, Oh S. Practical Synthesis of Hydroxychromenes and Evaluation of Their Biological Activity. Molecules. 2012; 17(1):240-247. https://doi.org/10.3390/molecules17010240

Chicago/Turabian Style

Jung, Jae-Chul; Oh, Seikwan. 2012. "Practical Synthesis of Hydroxychromenes and Evaluation of Their Biological Activity" Molecules 17, no. 1: 240-247. https://doi.org/10.3390/molecules17010240

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