3-pyrrolidin-3-yloxypyridine:hydrochloride synthesis

Yield:1219982-49-6 58%

Reaction Conditions:

with hydrogenchloride in 1,4-dioxane;dichloromethane at 20;Cooling;

Steps:

16.2

Ste 2: 3-(Pyrrolidin-3-yloxy)pyridine hydrochlorideTo a cooled solution of tart-butyl 3-(pyridin-3-yloxy)pyrrolidine-l-carboxylate (600 mg, 2.27 mmol; which may be prepared as described in Step 1) in dichloromethane (15 ml_) was added dropwise HCI 4N in dioxane (11.1 ml_). The solution was warmed to room temperature and stirred for 1 h. The solvent was evaporated under reduced pressure to give the title compound (263 mg, 58%) as a yellow wax. LCMS (ESI+) m/z 165 (M + H (-HCI))⁺ : 100%.

References:

WO2011/61214,2011,A1 Location in patent:Page/Page column 60