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

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.