反应详情

To a flask containing tert-butyl-3-((4-chloro-2-methoxy-3-(4-(trifluoromethyl)benzyl)quinolin-6-yl)(hydroxy)methyl)azetidine-1-carboxylate (525 mg, 0.98 mmol, Intermediate 61: step a) was added 1,4-dioxane (40 mL) to give a homogeneous solution at room temperature. Manganese dioxide (715 mg, 8.23 mmol) was then added and the mixture was heated to 85° C. in an aluminum heating mantle under nitrogen. After 60 minutes, the contents were filtered through a Celite® pad while the solution was still warm, rinsing with THF. The effluent was concentrated and purified by passing through a short column of silica gel (10% acetone-hexane increasing to 25% acetone) to provide the title compound as a white amorphous solid.

1. customto give a homogeneous solution at room temperature
2. filtrationthe contents were filtered through a Celite® pad while the solution
3. temperaturewas still warm
4. washrinsing with THF
5. concentrationThe effluent was concentrated
6. custompurified