反应详情

4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2-methoxyaniline (50 mg) was added to toluene (5 ml), and triethylamine (0.5 ml), and the mixture was heated under reflux to prepare a solution. A solution of triphosgene (50 mg) in methylene chloride was then added thereto, and the mixture was heated under reflux for 10 min. Next, 1-aminopiperidine (50 mg) was added thereto, and the mixture was further stirred with heating under reflux for 3 hr. A saturated aqueous sodium bicarbonate solution was added to the reaction solution to stop the reaction, and the reaction solution was then extracted with chloroform, followed by washing with water and saturated brine in that order. The organic layer was then dried over anhydrous sodium sulfate. The solvent was removed by distillation under the reduced pressure, and the residue was purified by HPLC using chloroform/methanol for development to give the title compound (43 mg, yield 62%).

1. temperaturethe mixture was heated
2. temperatureunder reflux
3. customto prepare a solution
4. temperaturethe mixture was heated
5. temperatureunder reflux for 10 min
6. temperaturewith heating
7. temperatureunder reflux for 3 hr
8. customthe reaction
9. extractionthe reaction solution was then extracted with chloroform
10. washby washing with water and saturated brine in that order
11. dry with materialThe organic layer was then dried over anhydrous sodium sulfate
12. customThe solvent was removed by distillation under the reduced pressure
13. customthe residue was purified by HPLC