Hydrochloric Acid → HCID 11857901, compound

Participants

Reaction Steps

To a solution of triphenylphosphine (0.81 g, 3.08 mmol, 1 eq) in dry tetrahydrofuran at 0° C. is added dropwise diisopropylazodicarboxylate (0.61 ml, 3.08 mmol, 1 eq). A solution of 2-fluoro-4-[4-(1-piperidinylmethyl)-1,3-oxazol-2-yl]phenol i68 (0.85 g, 3.08 mmol, 1 eq) and 3-(1-piperidinyl)-1-propanol (0.44 g, 3.08 mmol, 1 eq) in tetrahydrofuran is added dropwise to the mixture at 0° C. After 2 days, the mixture is poured onto 0.5 N hydrochloric acid and extracted with diethyl ether. The aqueous phase is basified with 1 N sodium hydroxide to pH 9 and extracted with ethyl acetate. The organic layer is dried on magnesium sulfate and concentrated under reduced pressure. The crude product is purified by chromatography over silica gel to afford 0.25 g of 1-(3-{2-fluoro-4-[4-(piperidin-1-ylmethyl)-1,3-oxazol-2-yl]phenoxy}propyl)piperidine 88 as a yellow oil.

Provenance & Evidence