反应详情

温度

60 °C

6-Bromo-N,N,5-trimethyl-3-oxo-4-[3-(trifluoromethyl)phenyl]-3,4-dihydropyrazine-2-carboxamide (0.10 g, 0.247 mmol), propargylaldehyde diethyl acetal (0.48 mg, 0.370 mmol), copper(I) iodide (0.001 mg, 0.005 mmol) and Et3N (1 ml) in THF (1 ml) were placed in a glass tube for microwave synthesis. The mixture was degassed with argon and Pd(Cl2) (PPh3)2 (0.007 g) was added. The tube was sealed and heated with stirring at 60° C. (150 W) in a microwave heater for 20 minutes. The mixture was diluted with EtOAc (5 ml) and filtered. The solution was concentrated in vacuo and was then purified on silica to give the title compound (28 mg, 25%).

1. customThe mixture was degassed with argon and Pd(Cl2) (PPh3)2 (0.007 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 then purified on silica