反应详情

温度

100 °C

3-(2-Fluoro-4-(methylsulfonyl)phenylamino)-1,4′-bipiperidin-2-one (0.300 g, 0.812 mmol), 2-chloro-5-ethylpyrimidine (0.116 g, 0.812 mmol) and DIEA (0.210 g, 1.62 mmol) were dissolved in DMF (5 mL) and heated at 100° C. overnight. The reaction was concentrated and purified over silica gel (50-100% EtOAc in hexanes) to provide 1′-(5-ethylpyrimidin-2-yl)-3-(2-fluoro-4-(methylsulfonyl)phenylamino)-1,4′-bipiperidin-2-one (0.198 g, 0.416 mmol, 51.3% yield) as white solid. Mass spectrum (apci) m/z=476.2 (M+H).

1. concentrationThe reaction was concentrated
2. custompurified over silica gel (50-100% EtOAc in hexanes)