反应详情

温度

70 °C

To a mixture of 1-(6-chloro-pyrazin-2-yl)-7-phenyl-2,3-dihydro-1H-imidazo[1,2-a]pyridin-5-one (85 mg, 0.26 mmol), sodium tert-butoxide (70 mg, 2.8 eq), BINAP (24 mg, 15% eq), and Pd (OAc)2 (9 mg, 15% eq) was added toluene (5 mL) and phenethylamine (39 μL, 1.2 eq). After purged with N2 for 10 min, the overall mixture was heated at 70° C. for 3 h prior to being cooled to room temperature. The resulting material was filtered through Celite and the filtrated cake was washed with DCM/MeOH (98:2) and the filtrates were concentrated. The residual material was purified by a preparative thin-layer chromatography (2% MeOH in DCM) to provide the title compound as a pale yellow solid. MS m/e 410 (M+H)+. Biological Assays

1. customAfter purged with N2 for 10 min
2. temperatureto being cooled to room temperature
3. filtrationThe resulting material was filtered through Celite
4. washthe filtrated cake was washed with DCM/MeOH (98:2)
5. concentrationthe filtrates were concentrated
6. customThe residual material was purified by a preparative thin-layer chromatography (2% MeOH in DCM)