反应详情

温度

110 °C

6-Bromo-N,5-dimethyl-3-oxo-4-[3-(trifluoromethyl)phenyl]-3,4-dihydropyrazine-2-carboxamide (SM2, 0.05 g, 0.128 mmol), 1-(4-cyanophenyl)-1H-pyrazol-5-boronic acid (SM4, 0.062 g, 0.256 mmol), Cs2CO3 (0.125 g, 0.384 mmol) and DME (3 ml) were added to a glass tube for microwave synthesis. The mixture was degassed with nitrogen and Pd(PBut3)2 (0.010 g) was added. The tube was sealed and heated with stirring at 110° C. (150 W) in a microwave heater for 10 minutes. The mixture was diluted with EtOAc (5 ml), and filtered. The solution was concentrated in vacuo and was purified by chromatography on silica to give a reasonably pure material that was further purified by preparative HPLC to give 0.012 g (20%) of the title compound as a white solid.

1. customThe mixture was degassed with nitrogen and Pd(PBut3)2 (0.010 g)
2. additionwas added
3. customThe tube was sealed
4. temperatureheated
5. additionThe mixture was diluted with EtOAc (5 ml)
6. filtrationfiltered
7. concentrationThe solution was concentrated in vacuo
8. customwas purified by chromatography on silica
9. customto give a reasonably pure material that
10. customwas further purified by preparative HPLC