反应详情

5-(3-[(1S)-2-Methoxy-1-methylethoxy]-5-{[6-(methylsulfonyl)pyridin-3-yl]oxy}phenyl)-1H-pyrrole-2-carboxylic acid (2.00 g, 4.48 mmol) synthesized in Example (78k) and (2R,3R)-3-aminobutan-2-ol (0.94 g, 8.96 mmol) synthesized in Example (88a) were dissolved in methanol (30 mL), and 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride n hydrate (2.84 g, 8.96 mmol) was added at room temperature, followed by stirring for 3 days under nitrogen atmosphere. The solvent was distilled off under reduced pressure, water (30 mL) was added, and the solution was separated with ethyl acetate (70 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=50%-90%) to afford the desired compound (1.33 g, 57%) as a white solid.

1. distillationThe solvent was distilled off under reduced pressure, water (30 mL)
2. additionwas added
3. customthe solution was separated with ethyl acetate (70 mL)
4. washThe organic layer was washed with saturated brine
5. dry with materialsubsequently dried over anhydrous magnesium sulfate
6. distillationThe solvent was distilled off under reduced pressure
7. customthe resulting residue was purified
8. washsilica gel column chromatography (elution solvent: ethyl acetate/hexane=50%-90%)