反应详情

To a solution of 5-[2-(2-chloro-4-hydroxy-phenyl)-1-hydroxy-1-trifluoromethyl-propyl]-1-methyl-1H-pyridin-2-one (Example 151, step 7, 100 mg) in N,N-dimethylacetamide (2 ml) were added 3,4-difluorobenzonitrile (46 mg) and cesium carbonate (272 mg). The mixture was stirred for 18 h at room temperature. EtOAc and ice water were added and the mixture was extracted with EtOAc. The organic phase was washed with water, dried (MgSO4), filtered and concentrated to dryness. The product was purified by chromatography (SiO2, cyclohexane/EtOAc 95:5=>0:1) to give the title compound (133 mg) as a colorless solid. MS (m/e)=481.1 [M+H+].

1. extractionthe mixture was extracted with EtOAc
2. washThe organic phase was washed with water
3. dry with materialdried (MgSO4)
4. filtrationfiltered
5. concentrationconcentrated to dryness
6. customThe product was purified by chromatography (SiO2, cyclohexane/EtOAc 95:5=>0:1)