(4-Boc-Amino-piperidin-1-yl)acetic acid ethylester synthesis

Yield:203662-91-3 490 mg

Reaction Conditions:

with potassium carbonate in N,N-dimethyl-formamide at 20;

Steps:

28.1 Step 1: Preparation of ethyl 2-(4-((tert-butoxycarbonyl)amino)piperidin-l-yl)acetate

To a mixture of tert-butyl piperidin-4-yl carbamate (500 mg, 2.49 mmol) in DMF (20 mL) were added ethyl 2-bromoacetate (500 mg, 2.99 mmol) and K₂C0₃(687 mg, 4.98 mmol). The mixture was stirred at r.t. overnight. Water (50 mL) was added, and the mixture was extracted with ethyl acetate (50 mL). The organic extract was washed with brine, dried over anhydrous Na₂S0₄, and evaporated under vacuum. The residue was purified by flash chromatography (silica gel, 1 % ~ 20 % ethyl acetate in petroleum ether) to give ethyl 2-(4- ((tert-butoxycarbonyl)amino)piperidin-l-yl)acetate (490 mg) as a white solid. LC-MS (ESI) found: 287 [M+l]⁺.

References:

WO2019/118612,2019,A1 Location in patent:Paragraph 0221