反应详情

4-(Piperidin-4-yl)-2H-isoquinolin-1-one hydrochloride (0.8 g) obtained in Example 31, potassium carbonate (2.0 g) and 2-bromoethanol (1.88 g) were dissolved in 2-butanone and water (1 mL), and the mixture was heated under reflux for 4 hrs. After the completion of the reaction, the solvent was evaporated, and water was added to the obtained residue. The mixture was extracted with chloroform, the organic layer dried over magnesium sulfate. The solvent was evaporated, and the obtained residue was purified by silica gel column chromatography (chloroform:methanol=4:1+triethylamine 2%) to give 4-(1-(2-hydroxyethyl)piperidin-4-yl)-2H-isoquinolin-1-one (0.46 g) as white crystals.

1. temperatureunder reflux for 4 hrs
2. customAfter the completion of the reaction
3. customthe solvent was evaporated
4. additionwater was added to the obtained residue
5. extractionThe mixture was extracted with chloroform
6. dry with materialthe organic layer dried over magnesium sulfate
7. customThe solvent was evaporated
8. customthe obtained residue was purified by silica gel column chromatography (chloroform:methanol=4:1+triethylamine 2%)