反应详情

1 M aqueous NaOH solution (1.15 mL) is added to a solution of methyl 2-((S)-6-((R)-4-(2,6-dimethyl-4-((3-methyloxetan-3-yl)methoxy)phenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetate (420 mg) in methanol (12 mL) at room temperature. The mixture is stirred at room temperature for 48 hours. The mixture is diluted with water and neutralized with 1 M aqueous HCl solution (1.15 mL). The resulting mixture is extracted with ethyl acetate, and the combined extract is washed with brine and dried (MgSO4). The solvent is evaporated and the residue is chromatographed on silica gel (cyclohexane/ethyl acetate 70:30→20:80). The product thus obtained is dissolved in acetonitrile/water (1:1) and lyophilized to give the title compound. Yield: 265 mg; LC (method 4): tR=1.87 min; Mass spectrum (ESI+): m/z=533 [M+H]+.

1. extractionThe resulting mixture is extracted with ethyl acetate
2. extractionthe combined extract
3. washis washed with brine
4. dry with materialdried (MgSO4)
5. customThe solvent is evaporated
6. customthe residue is chromatographed on silica gel (cyclohexane/ethyl acetate 70:30→20:80)
7. customThe product thus obtained