反应详情

温度

100 °C

Step R1-2: The mixture of 2-oxo-1,2,3,4-tetrahydroquinolin-7-yl trifluoromethanesulfonate (338 g), Zn(CN)2 (134 g) and Pd(PPh3)4 (33.5 g) in DMF (3.0 L) was heated at 100° C. for 4 hours and cooled to room temperature. To the mixture, Zn(CN)2 (134 g) and Pd(PPh3)4 (12.7 g) were added and the mixture was stirred at 100° C. for 2 hours. After cooling to 60° C., the reaction mixture was filtrated through a pad of Celite. The filtrate was concentrated to obtain a solid. The solid was washed with EtOAc twice to obtain 2-oxo-1,2,3,4-tetrahydroquinoline-7-carbonitrile as a pale yellow solid (165 g).

1. temperaturecooled to room temperature
2. temperatureAfter cooling to 60° C.
3. filtrationthe reaction mixture was filtrated through a pad of Celite
4. concentrationThe filtrate was concentrated
5. customto obtain a solid
6. washThe solid was washed with EtOAc twice