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63843-58-3

4-(4-BROMO-PHENOXY)-PIPERIDINE HYDROCHLORIDE synthesis

2synthesis methods
-

Yield:63843-58-3 71%

Reaction Conditions:

with hydrogenchloride in 1,4-dioxane;dichloromethane at 0 - 25; for 16 h;

Steps:

10.3 Step 3:

To a solution of Int-43 (30.5 mmol) in DCM (50 mL), was added HCI (4 N in dioxane, 22.85 mL, 91 mmol) in drop wise fashion at 0 °C. The resulting reaction mixture was stirred at 25 °C for 16 h. The reaction was followed by TLC, showed complete consumption of starting material. MTBE (50 mL) was added and stirring continued for 15 min. White solid precipitated, was filtered through a Buchner funnel. The solid was washed with hexane (50 mL) and dried under high vacuum to obtain 4-(4-bromophenoxy)piperidine hydrochloride (Int-44) as a white solid. Yield: 71%

References:

WO2022/173756,2022,A1 Location in patent:Paragraph 00288; 00290