反应详情

Under a nitrogen atmosphere a mixture of 6-chloro-N-[(1R)-1-phenylethyl]pyrazin-2-amine (0.611 g, 2.61 mmol), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol (0.785 g, 3.14 mmol), tetrakis(triphenylphosphine)palladium(0) (0.30 g, 0.26 mmol) and toluene (3 mL) was treated with 2M aqueous sodium carbonate solution (1.6 mL, 2.6 mmol). The resulting mixture was stirred vigorously whilst being heated under reflux for 24 hours. Once cool ethyl acetate was added and the mixture dried (MgSO4) and filtered. Removal of solvent in vacuo then yielded crude product, which was purified by column chromatography using dichloromethane:diethyl ether (99:1→90:10) as eluent: (0.619 g, 74%).

1. temperaturewhilst being heated
2. temperatureunder reflux for 24 hours
3. dry with materialthe mixture dried (MgSO4)
4. filtrationfiltered
5. customRemoval of solvent in vacuo
6. customthen yielded crude product, which
7. customwas purified by column chromatography