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Original Articles

Selective Anodic Monofluorination of Sulfur-Containing Heterocycles: Potent Applications towards Pharmaceuticals

Pages 343-344 | Published online: 17 Mar 2008
 

Abstract

Regioselective anodic monofluorination of 3-thiolanones, 1,3-oxathiolanones, and 1,3-dithiolanones was successfully carried out in MeCN containing Et3Nß3HF or Et4NFß4HF as a supporting electrolyte. Among the fluorinated products, 2-benzyl-4,4-dimethyl-2-ethoxycarbonyl-5-fluoro-3-thiolanone was found to possess comparable or even stronger in vitro human type II phospholipase A2 inhibitory activity compared with the known inhibitor, manoalide.

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