反应详情

温度

40 °C

A mixture of (4-{[4-difluoromethoxy-2-ethyl-8-fluoro-5-(2-methoxy-2-oxoethoxy) quinolin-3-yl]methyl}phenyl)boronic acid (0.1 g), 4-cyclopropyl-1H-pyrazole (0.047 g), cuprous acetate (0.078 g) and pyridine (3 mL) was heated at 40° C. for 24 hours. The mixture was cooled to room temperature, diluted with water (10 mL) and extracted with ethyl acetate. The combined extracts were washed with saturated aqueous sodium chloride solution, dried over magnesium sulphate and then concentrated under reduced pressure. Purification of the residue by column chromatography on silica gel, eluting with a mixture of cyclohexane and ethyl acetate (1:0 to 7:3 by volume) gave title compound as pale green oil (0.09 g).

1. temperatureThe mixture was cooled to room temperature
2. extractionextracted with ethyl acetate
3. washThe combined extracts were washed with saturated aqueous sodium chloride solution
4. dry with materialdried over magnesium sulphate
5. concentrationconcentrated under reduced pressure
6. customPurification of the residue by column chromatography on silica gel
7. washeluting with a mixture of cyclohexane and ethyl acetate (1:0 to 7:3 by volume)