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A Convenient Synthesis of the Echinacea-Derived Immunostimulator and HIV-1 Integrase Inhibitor (−)-(2R,3R)-Chicoric Acid

✍ Scribed by Anne-Marie Lamidey; Lionel Fernon; Laurent Pouységu; Charlotte Delattre; Stéphane Quideau; Patrick Pardon


Publisher
John Wiley and Sons
Year
2002
Tongue
German
Weight
87 KB
Volume
85
Category
Article
ISSN
0018-019X

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✦ Synopsis


The Echinacea-derived immunostimulator and HIV-1 integrase inhibitor (À)-chicoric acid ( 2,3-bis{[3-(3,4-dihydroxyphenyl)-1-oxoprop-2-enyl]oxy}butanedioic acid; 1a) was conveniently prepared via a silanepromoted Pd-mediated chemoselective hydrogenolysis of its perbenzylated derivative 12a, which was generated from an efficient and reliable carbodiimide-mediated coupling reaction between the caffeic acid dibenzyl ether derivative 7 and commercially available ()-dibenzyl l-tartrate (9a). The other naturally occurring dextrorotatory chicoric acid (1b) can be similarly prepared.