反应详情

温度

70 °C

Piperidine (0.747 mL) and paraformaldehyde (271 mg) were dissolved in acetic acid (3 mL), and the mixture was stirred at 70° C. for 5 min. 3-Methyl-2H-isoquinolin-1-one (302 mg) was added to the reaction mixture, and the mixture was heated under reflux for 2.5 hrs. After the completion of the reaction, the reaction mixture was concentrated, aqueous potassium carbonate solution was added. The mixture was extracted with chloroform, and the organic layer was dried over magnesium sulfate. The solvent was evaporated, and the obtained residue was purified by silica gel column chromatography (chloroform:methanol=20:1) to give 3-methyl-4-(piperidin-1-yl)methyl-2H-isoquinolin-1-one (99.3 mg).

1. temperaturethe mixture was heated
2. temperatureunder reflux for 2.5 hrs
3. customAfter the completion of the reaction
4. concentrationthe reaction mixture was concentrated
5. additionaqueous potassium carbonate solution was added
6. extractionThe mixture was extracted with chloroform
7. dry with materialthe organic layer was dried over magnesium sulfate
8. customThe solvent was evaporated
9. customthe obtained residue was purified by silica gel column chromatography (chloroform:methanol=20:1)