反应详情

温度

120 °C

7-methoxy-6-nitroquinazolin-4-ylamine (300 mg, 1.36 mmol) in <Step 6> of Example 23, 2-bromopyridine (0.2 mL, 2.04 mmol), palladium acetate (31 mg, 0.136 mmol), Xantphos (158 mg, 0.273 mmol) and cesium carbonate (888 mg, 2.73 mmol) were placed under 6.5 mL of 1,4-dioxane in a closed container, degassed, and the mixture was stirred at 120° C. for 2 hours. The mixture was cooled to room temperature, 50 mL water was added thereto, and the mixture was washed with a solution of chloroform/isopropanol (4:1). The mixture was dried over sodium sulfate and filtered and distilled under reduced pressure. The resulting oil was purified by column chromatography to obtain the title compound (78.5 mg, 20%).

1. customdegassed
2. temperatureThe mixture was cooled to room temperature
3. addition50 mL water was added
4. washthe mixture was washed with a solution of chloroform/isopropanol (4:1)
5. dry with materialThe mixture was dried over sodium sulfate
6. filtrationfiltered
7. distillationdistilled under reduced pressure
8. customThe resulting oil was purified by column chromatography