反应详情

温度

70 °C

A mixed solution of (2S)-2-(2-(((benzylcarbamoyl)amino)(prop-2-en-1-yl)amino)acetamido)-3-(4-(tert-butoxy)phenyl)-N-(2,2-diethoxyethyl)-N-((6-fluoropyridin-2-yl)methyl)propanamide (1.22 g, 1.73 mmol) described in Production Example 2-3 and formic acid (26 mL) was stirred at 70° C. for 3 hours. The reaction mixture was concentrated under a reduced pressure, water was added to the residue, and the resultant solution was extracted with ethyl acetate. An organic layer was washed with water and then with saturated brine, then dried over anhydrous magnesium sulfate, and then filtrated. The solvent was evaporated under a reduced pressure, and the resultant residue was purified by NH silica gel column chromatography (ethyl acetate:methanol=20:1) to give the title compound (865 mg, yield: 90%).

1. concentrationThe reaction mixture was concentrated under a reduced pressure, water
2. additionwas added to the residue
3. extractionthe resultant solution was extracted with ethyl acetate
4. washAn organic layer was washed with water
5. dry with materialwith saturated brine, then dried over anhydrous magnesium sulfate
6. filtrationfiltrated
7. customThe solvent was evaporated under a reduced pressure
8. customthe resultant residue was purified by NH silica gel column chromatography (ethyl acetate:methanol=20:1)