反应详情

4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2,3-dimethylaniline (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 (68 mg) in methylene chloride was then added thereto, and the mixture was heated under reflux for 10 min. Next, 2-(hydroxymethyl)-1,3-isoindolinedione (41 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 stop the reaction, and the reaction solution was then extracted with chloroform, followed by washing with a 1 N aqueous hydrochloric acid solution, water, and saturated brine in that order. The extract was dried over sodium sulfate and was then concentrated. The residue was purified on a column using chloroform/methanol to give the title compound (14 mg, yield 17%).

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 a 1 N aqueous hydrochloric acid solution, water, and saturated brine in that order
11. dry with materialThe extract was dried over sodium sulfate
12. concentrationwas then concentrated
13. customThe residue was purified on a column