反应详情

To a mixture of rac-3-[(2S,3S,4S)-2-(3-chloro-2-fluoro-phenyl)-3-(4-chloro-2-fluoro-phenyl)-3-cyano-4-(2,2-dimethyl-propyl)-pyrrolidin-1-yl]-propionic acid ethyl ester (12.3 mg, 0.0235 mmol) in THF (2 mL) was added a solution of LiOH (Aldrich, 6.7 mg, 0.16 mmol) in water (1 mL) and the reaction mixture was stirred at rt for 22 hrs. The reaction mixture was partly concentrated and quenched with 1 N HCl (pH 6-7), extracted with EtOAc, washed with water (2×), and saturated NaCl. The organic phase was separated, and dried over Na2SO4. The mixture was then concentrated to give rac-3-[(2S,3S,4S)-2-(3-chloro-2-fluoro-phenyl)-3-(4-chloro-2-fluoro-phenyl)-3-cyano-4-(2,2-dimethyl-propyl)-pyrrolidin-1-yl]-propionic acid (11 mg, 100%). HRMS (ES+) m/z Calcd for C25H26Cl2F2N2O2+H [(M+H)+]: 495.1412; Found: 495.1413.

1. concentrationThe reaction mixture was partly concentrated
2. customquenched with 1 N HCl (pH 6-7)
3. extractionextracted with EtOAc
4. washwashed with water (2×), and saturated NaCl
5. customThe organic phase was separated
6. dry with materialdried over Na2SO4
7. concentrationThe mixture was then concentrated