反应详情

To a solution of (S)-4,4-difluoro-2-[(morpholine-4-carbonyl)-amino]-5-phenyl-pentanoic acid methyl ester (2.81 g, 7.88 mmol) in MeOH:H2O (2:1 vol, 40 mL) is added LiOH mono hydrate (662 mg, 15.76 mmol). The mixture is stirred at room temperature for 2.5 h, and then diluted with water (30 mL). Methanol is removed in vacuum. The pH is adjusted to pH 1 with 6N HCl and the aqueous layer is extracted with dichloromethane (2×30 mL). The organic layers are dried over magnesium sulfate and concentrated in vacuum to afford (S)-4,4-Difluoro-2-[(morpholine-4-carbonyl)-amino]-5-phenyl-pentanoic acid (2.509 g, 93%).

1. customMethanol is removed in vacuum
2. extractionthe aqueous layer is extracted with dichloromethane (2×30 mL)
3. dry with materialThe organic layers are dried over magnesium sulfate
4. concentrationconcentrated in vacuum