Cyclopropanecarbonyl chloride → N-(6-Chloro-5-pyridin-4-ylpyrazin-2-yl)cyclopropanecarboxamide
反応式
[Cl:1][C:2]1[N:7]=[C:6]([NH2:8])[CH:5]=[N:4][C:3]=1[C:9]1[CH:14]=[CH:13][N:12]=[CH:11][CH:10]=1.[CH:15]1([C:18](Cl)=[O:19])[CH2:17][CH2:16]1>N1C=CC=CC=1>[Cl:1][C:2]1[N:7]=[C:6]([NH:8][C:18]([CH:15]2[CH2:17][CH2:16]2)=[O:19])[CH:5]=[N:4][C:3]=1[C:9]1[CH:14]=[CH:13][N:12]=[CH:11][CH:10]=1参加物
4
反応条件
- 温度
- 70 °C
実験手順
To a stirred solution of 6-chloro-5-pyridin-4-ylpyrazin-2-amine (Preparation 7, 0.73 g, 3.56 mmol) in pyridine (15 mL) was added cyclopropanecarbonyl chloride (648 μL, 7.1 mmol). The solution was stirred at 70° C. for 1 h 30 min, evaporated, partitioned between dichloromethane and a 4% sodium bicarbonate aqueous solution, the aqueous phase extracted twice with dichloromethane, the organic layers washed with brine, dried (MgSO4) and evaporated. The residue was triturated with diethyl ether and methanol and the precipitate was collected by filtration and dried to furnish the title compound as a light brown solid (0.69 g, 70%).