反应详情

To 1-{1-[5-amino-6-(methylamino)pyrimidin-4-yl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one (150 mg, 0.442 mmol) in acetonitrile (2 mL) was added camphorsulfonic acid (4.9 mg, 0.02 mmol) and trimethylorthoacetate (2 mL, 16.6 mmol). The mixture was heated at reflux for 15 h, then was cooled to ambient and was purified by preparative-HPLC to afford 1-[1-(8,9-dimethyl-9H-purin-6-yl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one as a beige solid (28 mg, 0.077 mmol, 17% yield).

1. temperatureThe mixture was heated
2. temperatureat reflux for 15 h
3. temperaturewas cooled to ambient and
4. customwas purified by preparative-HPLC