反应详情

温度

180 °C

260 mg (0.608 mmol) of 5-chloro-N-(3-{[3-fluoro-4-(3-oxo-4-morpholinyl)phenyl]-amino}-2-hydroxypropyl)-2-thiophenecarboxamide (from Example 61), 197 mg (1.22 mmol) of carbonylimidazole and 7 mg of dimethylaminopyridine are boiled in 20 ml of dioxane under reflux for 5 hours. 20 ml of acetonitrile are then added, and the mixture is stirred in a closed container in a microwave oven at 180° C. for 30 minutes. The solution is concentrated in a rotary evaporator and chromatographed on an RP-HPLC column. 53 mg (19% of theory) of the target compound are obtained.

1. temperatureunder reflux for 5 hours
2. concentrationThe solution is concentrated in a rotary evaporator
3. customchromatographed on an RP-HPLC column
4. custom53 mg (19% of theory) of the target compound are obtained