反应详情

1-Cyclopentyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-(trans-4-hydroxy-cyclohexylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one was prepared as in Example 2 using 0.5 g (1.15 mmol) 1-cyclopentyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-methanesulfinyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one and 0.389 g (3.45 mmol) trans-4-hydroxy-cyclohexylamine. The final product was purified by column chromatography (20:1 dichloromethane/ methanol). This gave 0.320 g (57%) of 1-cyclopentyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-(trans-4-hydroxy-cyclohexylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one as a white solid: mp 108° C.–110° C.; MS (APCI) m/z 486.2, 487.2.

1. customThe final product was purified by column chromatography (20:1 dichloromethane/ methanol)