反应详情

To a solution of (4RS,5SR)-5-(4-fluorophenyl)-4-((3-(2,2,2-trifluoroethoxy)phenyl)methyl)-1,3-oxazolidin-2-one (1.2 g, 3.25 mmol) in ethanol (10 ml) was added 8N aqueous sodium hydroxide solution (2.0 ml, 16 mmol) and the mixture was heated under reflux for 2 hrs. The reaction solution was concentrated, diluted with water (100 ml) and extracted with ethyl acetate (100 ml×2). The extract was washed with saturated brine, dried over anhydrous magnesium sulfate and evaporated under reduced pressure. The residue was recrystallized from ethyl acetate-hexane to give (1RS,2SR)-2-amino-1-(4-fluorophenyl)-3-(3-(2,2,2-trifluoroethoxy)phenyl)-1-propanol (913 mg, 82%).

1. temperaturethe mixture was heated
2. temperatureunder reflux for 2 hrs
3. concentrationThe reaction solution was concentrated
4. additiondiluted with water (100 ml)
5. extractionextracted with ethyl acetate (100 ml×2)
6. washThe extract was washed with saturated brine
7. dry with materialdried over anhydrous magnesium sulfate
8. customevaporated under reduced pressure
9. customThe residue was recrystallized from ethyl acetate-hexane