反应详情

The 7-(5-aminomethyl-2-oxooxazolidin-3-yl)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one (15.3 mg, 0.038 mmol) obtained in Example 1-31 was dissolved in pyridine (380 μl). Thereafter, acetyl chloride (3.2 μl) was added to the obtained solution, and the obtained mixture was stirred at a room temperature for 2 hours. Thereafter, 1 N hydrochloric acid was added to the reaction solution under cooling on ice, followed by extraction with ethyl acetate. The extract was dried over anhydrous sodium sulfate, and the solvent was then distilled away under reduced pressure. The obtained residue was purified by silica gel column chromatography (methylene chloride:methanol=20:1), so as to obtain N-{2-oxo-3-[1-oxo-3-(2-trifluoromethylphenyl)-1,2-dihydroisoquinolin-7-yl]oxazolidin-5-ylmethyl}acetamide (12.1 mg; yield: 71%) in the form of a colorless amorphous substance.

1. temperatureunder cooling on ice
2. extractionfollowed by extraction with ethyl acetate
3. dry with materialThe extract was dried over anhydrous sodium sulfate
4. distillationthe solvent was then distilled away under reduced pressure
5. customThe obtained residue was purified by silica gel column chromatography (methylene chloride:methanol=20:1)