反应详情

LiOH×H2O (38 mg) is added to a solution of methyl 2-((S)-6-((R)-4-(4-cyano-2,6-dimethylphenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetate (85 mg) in tetrahydrofuran (1 mL), water (1 mL) and methanol (1 mL) at room temperature. The mixture is stirred at room temperature for 12 hours. The mixture is concentrated, cooled to 0° C., diluted with water and acidified with 4 M aqueous HCl solution. The resulting mixture is extracted with dichloromethane. The organic phase is dried (MgSO4). The solvent is evaporated and the residue is chromatographed on silica gel (dichloromethane/methanol/acetic acid 9:0.05:0.05) to give the title compound. Yield: 41 mg; LC (method 20): tR=6.91 min; Mass spectrum (ESI−): m/z=456 [M−H]−.

1. concentrationThe mixture is concentrated
2. temperaturecooled to 0° C.
3. additiondiluted with water
4. extractionThe resulting mixture is extracted with dichloromethane
5. dry with materialThe organic phase is dried (MgSO4)
6. customThe solvent is evaporated
7. customthe residue is chromatographed on silica gel (dichloromethane/methanol/acetic acid 9:0.05:0.05)