反应详情

Methyl (4S)-2-[5-(3-[(1S)-2-methoxy-1-methylethoxy]-5-{[6-(methylsulfonyl)pyridin-3-yl]oxy}phenyl)-1H-pyrrol-2-yl]-4,5-dihydro-1,3-oxazole-4-carboxylate (1.76 g, 3.32 mmol) synthesized in Example (86b) was dissolved in tetrahydrofuran (30 mL), and lithium aluminum hydride (0.25 g, 6.65 mmol) was added at 0° C. After stirring for 30 minutes under nitrogen atmosphere, water (0.25 mL), a 5N aqueous sodium hydroxide solution (0.25 mL) and water (0.75 mL) were added in this order, and stirring was carried out for 10 minutes. Ethyl acetate (100 mL) was added followed by stirring for 5 minutes, and subsequently drying was carried out 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: methanol/methylene chloride=0%-5%) to afford the desired compound (1.15 g, 69%) as a white powder.

1. stirringstirring
2. waitwas carried out for 10 minutes
3. stirringby stirring for 5 minutes
4. customsubsequently drying
5. distillationThe solvent was distilled off under reduced pressure
6. customthe resulting residue was purified
7. washsilica gel column chromatography (elution solvent: methanol/methylene chloride=0%-5%)