反应详情

温度

100 °C

(S)-3-(2,5-difluoro-4-(methylsulfonyl)phenylamino)-1,4′-bipiperidin-2-one hydrochloride (2.6 g, 6.1 mmol) was dissolved in DMF (30 mL) and DIEA (3.2 mL, 18 mmol) and 2-chloro-5-ethylpyrimidine (1.1 g, 8.0 mmol) were added and heated at 100° C. overnight. The reaction was concentrated and purified over silica gel (25-100% EtOAc in hexanes) to afford (S)-3-(2,5-difluoro-4-(methylsulfonyl)phenylamino)-1′-(5-ethylpyrimidin-2-yl)-1,4′-bipiperidin-2-one (1.5 g, 3.1 mmol, 51% yield) as a white solid. Mass spectrum (apci) m/z=494.3 (M+H).

1. concentrationThe reaction was concentrated
2. custompurified over silica gel (25-100% EtOAc in hexanes)