反应详情

To a solution of tert-butyl 2-{2-[(1R,5S)-3-(2-methyl-1H-benzimidazol-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]ethyl}-2-phenylmorpholine-4-carboxylate (330 mg, 0.62 mmol) in 5 mL CHCl3 was added 0.8 mL of a solution of 4N HCl in dioxane. After stirring at room temperature for 2 h, another 3 mL 4N HCl in dioxane was added and the mixture was heated at 40° C. for 90 min. The solution was then evaporated and dried in vacuo to provide 2-methyl-1-{(1R,5S)-8-[2-(2-phenylmorpholin-2-yl)ethyl]-8-azabicyclo[3.2.1]oct-3-yl}-1H-benzimidazole trihydrochloride, which was used without further purification. ESI-MS 431 (M+H).

1. temperaturethe mixture was heated at 40° C. for 90 min
2. customThe solution was then evaporated
3. customdried in vacuo