Antipicomavirus agent

Lemiere and coworkers synthesized the antipicomavirus agent 3-0-Methylquercetin (76). A key transformation was the conversion of acetophenone 61a to 3-methoxyflavone 79. In the event, 61a and 3,4-dibenzyloxybenzoic anhydride (77) were allowed to react at 160 C in the presence of sodium carboxylate 78 to deliver the penultimate intermediate in 78% yield. Debenzylation of 79 in the presence of Pearlman s catalyst delivered the natural product in 99% yield. 

Otto MJ, Fox MP, Fancher MJ, Kuhrt MF, Diana GD, McKinlay MA. In vitro activity of WIN 51711, a new broad spectrum antipicomavirus agent. Antimicrob Agents Chemother 1985 27 883-886. 

ISHiTSUKA et aL screened natural products for antirhinoviral activity and reported that a flavone (Ro 09-0179), a potent antipicomavirus agent, was isolated from a Chinese medicinal herb (Agastache rugosa Kuntze) (173). We studied the antiviral effects on rhinovirus type 2 and found that morusin hydroperoxide (49), oxydihydromorusin (34), chalcomoracin (103), and compound A (31) had marginal anti-rhino viral activities (MIC, 1.25-2.5 ig/ml) (48). 

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