反应详情

132.6 μl (20 mmol) of (R)-glycidol was added to an ethanol solution (10 ml) containing 608.5 mg (2.0 mmol) of the 7-amino-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one obtained in Example 38. The obtained mixture was stirred under heating to reflux overnight. The residue obtained by concentration of the reaction solution was purified by silica gel column chromatography (methylene chloride:methanol=20:1), so as to obtain 514.3 mg (68%) of 7-((S)-2,3-dihydroxypropylamino)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one in the form of a light yellow amorphous substance.

1. temperatureunder heating
2. temperatureto reflux overnight
3. customThe residue obtained by concentration of the reaction solution
4. customwas purified by silica gel column chromatography (methylene chloride:methanol=20:1)