反应详情

温度

50 °C

To a solution of (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (310 mg) and 2-chloro-5-nitropyridine (205 mg) in DMSO (2 ml) was added cesium carbonate (423 mg). The mixture was stirred at 50° C. for 5 h. The solvent was evaporated, the residue was dissolved in EtOAc and washed with water (2×) and brine (1×). The organic phase was dried, filtered and concentrated. The product was purified by flash chromatography (cyclohexane/EtOAc 9:1=>4:6) to give (RS)-N-[4-cyano-2-(5-nitro-pyridin-2-yloxy)-benzyl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide. Light yellow foam. MS 481.4 ([M+H]+)

1. customThe solvent was evaporated
2. dissolutionthe residue was dissolved in EtOAc
3. washwashed with water (2×) and brine (1×)
4. customThe organic phase was dried
5. filtrationfiltered
6. concentrationconcentrated
7. customThe product was purified by flash chromatography (cyclohexane/EtOAc 9:1=>4:6)