反应详情

To a solution of 7-bromo-6-fluoro-1H-indole (D140) (1.0 g) in DMF (15 ml) were added Zn(CN)2 (2.2 g) and then Pd(PPh3)4 (1.1 g) in a microwave tube, then N2 atmosphere was bubbled in. The sealed vial was irradiated in the microwave at 150° C. for 2 hours. After cooling, DCM (80 mL) was added to the resulting mixture which was filtered and the filtrate was concentrated. The crude product was purified by column chromatography to afford 6-fluoro-1H-indole-7-carbonitrile (D141) (0.5 g) as a white solid.

1. customPd(PPh3)4 (1.1 g) in a microwave tube, then N2 atmosphere was bubbled in
2. customThe sealed vial was irradiated in the microwave at 150° C. for 2 hours
3. temperatureAfter cooling
4. additionDCM (80 mL) was added to the resulting mixture which
5. filtrationwas filtered
6. concentrationthe filtrate was concentrated
7. customThe crude product was purified by column chromatography