反应详情

(R)-Glycidol (78.3 μl, 1.18 mmol) was added to an ethanol solution (4 ml) that contained the 7-amino-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one obtained in step C of Example 1-1, and the obtained mixture was stirred under heating to reflux for 3 days. Thereafter, the reaction solution was concentrated under reduced pressure, and the obtained residue was purified by silica gel column chromatography (methylene chloride:methanol=20:1), so as to obtain 7-((S)-2,3-dihydroxypropylamino)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one (281.9 mg; yield: 63%) in the form of a pale yellow amorphous substance.

1. temperatureunder heating
2. temperatureto reflux for 3 days
3. concentrationThereafter, the reaction solution was concentrated under reduced pressure
4. customthe obtained residue was purified by silica gel column chromatography (methylene chloride:methanol=20:1)