1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(methylsulfinyl)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one → 1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-(4-hydroxy-cyclohexylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one

Participants

Reaction Conditions

Reaction Steps

To a solution of 0.511 g (1.13 mmol) of 1-cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-methylsulfinyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one was added 0.39 g (3.39 mmol) of trans-4-aminocyclohexanol. The resulting mixture was heated at 1 10° C. oil bath temperature for 2 days under N2 atmosphere. The dioxane was evaporated. The crude product was purified by medium-pressure chromatography eluting with 20:1 dichloromethane/methanol to give 0.50 g (88%) of title compound: mp 208° C.–212° C. (dec). MS (APCI) (m+1)/z 504.2.

Provenance & Evidence