反应详情

An oven dried resealable Schlenk tube was charged with 6-(3-fluorophenyl)-5-pyridin-4-ylpyrazin-2-amine (Example 1, 100 mg, 0.37 mmol), 3-bromopyridine (43 μL, 0.45 mmol), 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene (17 mg, 0.03 mmol), cesium carbonate (171 mg, 0.52 mmol) and dioxane (2 mL). The Schlenk tube was subjected to three cycles of evacuation-backfilling with argon, and tris(dibenzilideneacetone) dipalladium (14 mg, 0.01 mmol) was added. After three new cycles of evacuation-backfilling with argon, the Schlenk tube was capped and placed in a 100° C. oil bath. After 20 h, the mixture was cooled and water was added. The solid was collected by filtration, washed with water, diethyl ether and dried, to give the title compound as a yellow solid (88 mg, 63%).

1. customAn oven dried resealable Schlenk tube
2. additionwas added
3. customAfter three new cycles of evacuation-backfilling with argon, the Schlenk tube was capped
4. customplaced in a 100° C.
5. temperaturethe mixture was cooled
6. filtrationThe solid was collected by filtration
7. washwashed with water, diethyl ether
8. customdried