反应详情

温度

40 °C

To a mixture of N-(3-fluoro-4-(7-hydroxyquinolin-4-yloxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (735.7 mg, 1.52 mmol) and 2-(1-hydroxycyclopropyl)ethyl methanesulfonate (3.04 mmol) in 8 mL of N,N-dimethylacetamide was added cesium carbonate (4.955 g, 15.2 mmol). After stirring at 40° C. for 1 day, the reaction was quenched with water (5 mL) and extracted with CH2Cl2 (20 mL×3). The combined organic phases were dried over Na2SO4 and concentrated in vacuo. The residue was chromatographed on a silica gel column (CH2Cl2/CH3OH (v/v)=45:1) to afford the title compound as a white solid (270 mg, 15.6%).

1. customthe reaction was quenched with water (5 mL)
2. extractionextracted with CH2Cl2 (20 mL×3)
3. dry with materialThe combined organic phases were dried over Na2SO4
4. concentrationconcentrated in vacuo
5. customThe residue was chromatographed on a silica gel column (CH2Cl2/CH3OH (v/v)=45:1)