Triethylamine → 3-methyl-2-((2S)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)morpholino)-6-(pyrimidin-4-yl)pyrimidin-4(3H)-one

Participants

Reaction Steps

To a solution of 2-chloro-3-methyl-6-(pyrimidin-4-yl)-3H-pyrimidin-4-one (intermediate 1, 12.6 g, 56.6 mmol) and (2S)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)morpholine hydrochloride (intermediate 19, 16.7 g, 59.3 mmol) was added triethylamine (17.2 g, 170 mmol) at room temperature and the mixture was stirred at room temperature for 8 hours. The organic solvent was removed under reduced pressure, and the resulting crude product was washed with ethyl acetate and water and dried under reduced pressure to afford 3-methyl-2-((2S)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)morpholino)-6-(pyrimidin-4-yl)pyrimidin-4(3H)-one (compound of the present invention, 23.7 g, 97%).

Provenance & Evidence