反应详情

温度

60 °C

1-(4-{[3-(Hydroxymethyl)cyclobutyl]oxy}phenyl)-N-pyridin-3-ylmethyl-1H-benzimidazole-5-carboxamide (33 mg, 0.08 mmol) was dissolved in DMF and put under N2 atmosphere. Sodium hydride (2 mg, 0.08 mmol) was added and the reaction was heated to 60° C. 2-Fluoropyridine was then added and the reaction was then heated to 80° C. for 14 h. The reaction was cooled to rt and concentrated in vacuo. The crude solid was purified using the Waters mass-directed HPLC purification system to provide 1-(4-{[3-(2-pyridyloxymethyl)cyclobutyl]oxy}phenyl)-N-pyridin-3-ylmethyl-1H-benzimidazole-5-carboxamide as an off-white solid. MS (ES+): m/z 507 (10) [MH+].

1. temperaturethe reaction was then heated to 80° C. for 14 h
2. temperatureThe reaction was cooled to rt
3. concentrationconcentrated in vacuo
4. customThe crude solid was purified
5. customthe Waters mass-directed HPLC purification system