反应详情

A mixture of intermediate 1 (Example 2) (40 mg, 1.2 mmol) and thionyl chloride (875 μL, 12 mmol) in dichloromethane (20 mL) was heated under reflux for 6 h. The reaction mixture was evaporated to dryness. To the residue was added (4-(5-aminopyrimidin-2-ylamino)phenyl)(4-methylpiperazin-1-yl)methanone (20 mg, 0.064 mmol) and TEA (44 μL, 0.31 mmol) in THF (7 mL). The reaction mixture was stirred at room temperature for 1 h and evaporated. The residue was purified by HPLC to give title compound as a yellow solid (21 mg, 52%).

1. temperaturewas heated
2. temperatureunder reflux for 6 h
3. customThe reaction mixture was evaporated to dryness
4. customevaporated
5. customThe residue was purified by HPLC