2-(Dimethylamino)ethanol → (5-{7-[2-(2-Dimethylaminoethoxy)-pyridin-4-yl]-2-morpholin-4-yl-6,7-dihydro-5h-pyrrolo[2,3-d]pyrimidin-4-yl}-pyrimidin-2-yl)-bis-(4-methoxy-benzyl)-amine

Participants

Reaction Steps

Sodium hydride (15 mg, 60% mineral oil dispersion, 5 equivalents) and N,N-dimethylaminoethanol (39 μl, 5 equivalents) were added to toluene (1.3 ml). After refluxing for 5 minutes, stirring was carried out at 50° C. for 15 minutes. {5-[7-(2-Chloro-pyridin-4-yl)-2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrimidin-2-yl}-bis-(4-methoxy-benzyl)-amine (50 mg) obtained in Step A in Example 1-H-31 was added, followed by refluxing overnight, and the reaction mixture was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (dichloromethane/methanol=30/1 to 10/1), to obtain a colorless solid (54 mg, 100%).

Provenance & Evidence