Water → HCID 16662172, compound

Participants

Reaction Steps

(5S)-5-(azepan-1-ylmethyl)-1-{4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl}pyrrolidin-2-one 20 (0.1 g, 0.24 mmol, 1 eq) is dissolved in chloroform (5 ml) and 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-disulfide a49 (Lawesson's reagent, 0.05 g, 0.12 mmol, 0.5 eq) is added. Toluene (5 ml) is added and the mixture is refluxed for 6 h. Water is then added, and after phase separation, the organic layer is dried over magnesium sulfate and concentrated to give 0.2 g of crude material. Purification by chromatography over silicagel (dichloromethane/methanol/ammonia 94/6/0.6) affords 0.05 g of pure (5S)-5-(azepan-1-ylmethyl)-1-{4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl}pyrrolidine-2-thione 21.

Provenance & Evidence