反应详情

N,N-Dimethylformamide (2 ml) was added to 4-[4-(4-tert-butylphenylamino)phenoxy]-6-methoxyquinolin-7-ol (compound 21) (150 mg) (starting compound A) and potassium carbonate (250 mg). Epibromohydrin (46 μl) was added dropwise thereto, and the mixture was stirred at room temperature for 24 hr. Morpholine (95 μl) (starting compound B) was added dropwise to the reaction solution, and the mixture was stirred at 70 to 75° C. for 5 hr. The stirred mixture was extracted with ethyl acetate, and the extract was washed with saturated brine and was dried over sodium sulfate. The solvent was then removed by evaporation under the reduced pressure. The crude thus obtained was purified by thin-layer chromatography on silica gel using chloroform/methanol for development to give the title compound (179 mg, yield 89%).

1. stirringthe mixture was stirred at 70 to 75° C. for 5 hr
2. extractionThe stirred mixture was extracted with ethyl acetate
3. washthe extract was washed with saturated brine
4. dry with materialwas dried over sodium sulfate
5. customThe solvent was then removed by evaporation under the reduced pressure
6. customThe crude thus obtained
7. customwas purified by thin-layer chromatography on silica gel