tert-butyl 6-acetyl-2,6-diazaspiro[3.3]heptane-2-carboxylate synthesis

Yield:1349875-71-3 78%

Reaction Conditions:

with potassium hydroxide in dichloromethane at 20; for 1 h;

Steps:

40.1

To a solution of 2,6-diaza-spiro[3.3]heptane-2-carboxylic acid tert-butyl ester (130) (purchased from WUXI APPTEC^} ((500 mg, 2.73 mmol) in CH₂C1₂ (10 mL) were added KOH (459 mg, 8.19 mmol) and Ac₂0 (279 mg, 2.73 mmol). The reaction mixture was stirred at RT for 1 h, then diluted with CH₂C1₂ (20 mL), washed with H₂0 (20 mL). The organic layer was washed with brine (20 mL), dried over Na₂S0₄, and filtered, evaporated to give the product (131) (510 mg, 2.13 mmol, yield: 78%). ESI-MS (M+l): 241 calc. for Ci₂H₂oN₂0₃ 240.

References:

WO2011/143365,2011,A1 Location in patent:Page/Page column 193