反应详情

A suspension of 6-cyano-2-chloropyrazine (0.3 g, 2.1 mmol), (1,1′-bis(diphenylphosphino)ferrocene)-dichloropalladium (II) (153.6 mg, 0.21 mmol), potassium phosphate (1.3 g, 6.30 mmol) and cyclopropylboronic acid (0.184 mg, 2.1 mmol) in tetrahydrofuran (25 mL, nitrogen bubbled) was degassed for 15 min. using nitrogen. The reaction mixture was refluxed for 16 h. The reaction mixture was filtered through Celite and the filtrate was concentrated under reduced pressure. The crude material was purified via column chromatography (100-200 mesh silica gel, 5-20% ethyl acetate in petroleum ether) to afford 6-cyclopropylpyrazine-2-carbonitrile (250 mg, 50%).

1. customwas degassed for 15 min.
2. temperatureThe reaction mixture was refluxed for 16 h
3. filtrationThe reaction mixture was filtered through Celite
4. concentrationthe filtrate was concentrated under reduced pressure
5. customThe crude material was purified via column chromatography (100-200 mesh silica gel, 5-20% ethyl acetate in petroleum ether)