反应详情

A solution of KOH (113.6 mg, 2.04 mmol) in EtOH (2 mL) was added dropwise to a solution of 2-[1-(6-tert-butoxycarbonylamino-pyridin-3-yl)-ethyl]-malonic acid diethyl ester (0.7 g, 1.84 mmol) in methylene chloride (4 mL) and EtOH (10 mL) at 0° C. under argon and the reaction mixture was stirred over night. 1M KOH (100 mL) was added and the mixture was washed with methylene chloride. The aqueous phase was acidified to pH 2 using 2 M HCl and extracted with EtOAc. The organic phase was dried and concentrated under reduced pressure to give the crude 2-[1-(6-tert-butoxycarbonylamino-pyridin-3-yl)-ethyl]-malonic acid monoethyl ester (423 mg, 65%).

1. washthe mixture was washed with methylene chloride
2. extractionextracted with EtOAc
3. customThe organic phase was dried
4. concentrationconcentrated under reduced pressure