反应详情

N-[(2S)-2,3-Dihydroxypropyl]-5-{3-[(1S)-2-methoxy-1-methylethoxy]-5-[4-(methylsulfonyl)phenoxy]phenyl}-1H-pyrrole-2-carboxamide (265 mg, 0.514 mmol) synthesized in Example (35a) was dissolved in dichloromethane (10 mL), and triisopropylsilyl chloride (0.12 mL, 0.691 mmol), triethylamine (0.21 mL, 1.51 mmol) and 4-dimethylaminopyridine (6.0 mg, 0.049 mmol) were added, followed by stirring at room temperature for 24 hours under nitrogen atmosphere. Water (10 mL) was added, and the solution was separated with dichloromethane (20 mL). The organic layer was washed with saturated brine, and subsequently dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was purified using silica gel column chromatography (elution solvent: ethyl acetate/hexane=20%-50%) to afford the desired product (177 mg, yield 51%) as a white solid.

1. customthe solution was separated with dichloromethane (20 mL)
2. washThe organic layer was washed with saturated brine
3. dry with materialsubsequently dried over anhydrous magnesium sulfate
4. distillationThe solvent was distilled off under reduced pressure
5. customthe resulting residue was purified
6. washsilica gel column chromatography (elution solvent: ethyl acetate/hexane=20%-50%)