反应详情

Under argon, (4R)-4-(4-cyano-2-nitrophenyl)-6-methyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (39.5 g, 92.4 mmol) was dissolved in ethanol (1975 ml). 10% Palladium on activated carbon (19.8 g) was then added, and the mixture was hydrogenated at RT and atmospheric pressure for 2 h (strictly monitored by TLC). The reaction mixture was then filtered through kieselguhr. The filtrate was concentrated and the crude product obtained was subjected to flash chromatography on silica gel (mobile phase: ethyl acetate/cyclohexane 2:1). The title compound was obtained as a solid (25.5 g, 68% of theory).

1. customwas hydrogenated at RT
2. filtrationThe reaction mixture was then filtered through kieselguhr
3. concentrationThe filtrate was concentrated
4. customthe crude product obtained