反应详情

To a solution of tert-butyl 4-(4-carbamoyl-3-{[4-(2-methoxy-2-oxoethyl)phenyl]amino}-1H-pyrazol-1-yl)-4-(cyanomethyl)piperidine-1-carboxylate (Example 12-2) (0.10 g, 0.20 mmol) in THF (1.0 mL) was added a solution of LiOH (19 mg, 0.81 mmol) in water (0.8 mL). The mixture was stirred at ambient temperature for 2 hours. The mixture was then neutralized with 1N aqueous HCl to pH 3-4, diluted with water, and extracted with EtOAc. The organic layer was separated, washed with brine, dried over anhydrous MgSO4, and concentrated in vacuo. The residue was purified by MPLC on silica gel (using a gradient elution of 0-10% MeOH/EtOAc) to afford the title compound, Example #18.

1. extractionextracted with EtOAc
2. customThe organic layer was separated
3. washwashed with brine
4. dry with materialdried over anhydrous MgSO4
5. concentrationconcentrated in vacuo
6. customThe residue was purified by MPLC on silica gel (
7. washa gradient elution of 0-10% MeOH/EtOAc)