反应详情

温度

30 °C

Methyl (1-{2-[2-(2-oxopiperidin-1-yl)phenyl]ethyl}pyrrolidin-3-yl)acetate a13-1 (500 mg, 0.87 mmol, 1 eq) is dissolved in MeOH/H2O (4 ml/1 ml) and LiOH (47 mg, 1.7 mmol, 2 eq) is added. The reaction mixture is stirred at 30° C. for 1 hour, then quenched with HCl 1M (100 μl). The resulting mixture is diluted with n-butanol (15 ml), and stirred overnight at room temperature. After phase separation the organic layer is dried on Na2SO4, filtered and the filtrate is concentrated under reduced pressure to afford 229 mg of (1-{2-[2-(2-oxopiperidin-1-yl)phenyl]ethyl}pyrrolidin-3-yl)acetic acid a14-1 as a colorless oil which is used in the next step without any further purification.

1. customquenched with HCl 1M (100 μl)
2. additionThe resulting mixture is diluted with n-butanol (15 ml)
3. stirringstirred overnight at room temperature
4. customAfter phase separation the organic layer
5. customis dried on Na2SO4
6. filtrationfiltered
7. concentrationthe filtrate is concentrated under reduced pressure