反应详情

30% Aqueous NH3 solution (250 μL) and 35% aqueous H2O2 solution (83 μl) are added at 0° C. to a solution of 2-((S)-6-((R)-4-(4-cyano-2,6-dimethylphenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetic acid (19 mg) in ethanol (2 mL). The mixture is stirred at room temperature for 12 hours, while warming to room temperature. The mixture is concentrated, diluted with water and neutralized with 4 M aqueous HCl solution. The resulting mixture is extracted with dichloromethane. The organic phase is dried (MgSO4). The solvent is evaporated to give the title compound. Yield: 19 mg; LC (method 20): tR=5.33 min; Mass spectrum (ESI+): m/z=476 [M+H]+.

1. temperaturewhile warming to room temperature
2. concentrationThe mixture is concentrated
3. additiondiluted with water and neutralized with 4 M aqueous HCl solution
4. extractionThe resulting mixture is extracted with dichloromethane
5. dry with materialThe organic phase is dried (MgSO4)
6. customThe solvent is evaporated