1-(propylsulfonyl)-3-Azetidinol synthesis

Yield:-

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine in dichloromethane at 0 - 20;

Steps:

83.1

83.1 1 -(Propane-1 -sulfonyl)-azetidin-3-ol; To a cooled solution (0-5⁰C) of azetidin-3-ol hydrochloride (1 g, 9,13 mmol) in 10 ml di- chloromethane containing diisopropyl ethyl amine (2,391 ml, 13,69 mmol) was added dropwise a solution of propane-1 -sulfonyl chloride (1 ,126 ml, 10,04 mmol) dissolved in 5 ml dichloromethane over an 1 h period. The mixture was allowed to warm up to room temperature and was stirred over night. Citric acid (10%) was added, extracted with dichloromethane, dried over MgSO₄, filtered and the solvent was evaporated to obtain 597 mg of a yellow oil, which was purified by chromatography (yield 470 mg)

References:

WO2010/92180,2010,A1 Location in patent:Page/Page column 139