Lithium Hydroxide → (1-{2-[2-(2-Oxopiperidin-1-yl)phenyl]ethyl}pyrrolidin-3-yl)acetic acid

Participants

Reaction Conditions

Reaction Steps

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.

Provenance & Evidence