反应详情

To a solution of (2S)-2-(4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)morpholine hydrochloride (intermediate 13, 4.00 g, 14.2 mmol) and 1H-pyrazole-1-carboxamidine hydrochloride (2.19 g, 14.9 mmol) in N,N-dimethylformamide (14 ml) was added. N,N-diisopropylethylamine (4.05 g, 31.3 mmol) at room temperature and the solution was stirred for 4 hours. The solution was decanted with ether, then 3-oxo-3-pyrimidin-4-yl-propionic acid ethyl ester (3.59 g, 18.5 mmol), potassium carbonate (4.92 g, 35.6 mmol) and ethanol (30 ml) were added to the resulting solution. After refluxed for 18 hours, the solution was concentrated under reduced pressure. The residue was washed with water and the hot mixture of ethanol and 1N hydrochloric acid (1/1, v/v), and dried under reduced pressure to afford 2-{(2S)-2-[4-(5-methyl-[1,2,4]oxadiazol-3-yl)-phenyl]-morpholin-4-yl}-1H-[4,4′]bipyrimidinyl-6-one (1.94 g, 33%).

1. customThe solution was decanted with ether
2. temperatureAfter refluxed for 18 hours
3. concentrationthe solution was concentrated under reduced pressure
4. washThe residue was washed with water
5. additionthe hot mixture of ethanol and 1N hydrochloric acid (1/1
6. customv/v), and dried under reduced pressure