反应详情

To a solution of 2-(5,7-difluoroquinolin-6-ylmethyl)isoindoline-1,3-dione (5.10 g, 15.73 mmol) in CH3OH (150 mL) was added hydrazine monohydrate (0.50 g, 15.73 mmol). The solution was heated at reflux for 3 h. After cooling, the mixture was filtered through celite. The filtrate was concentrated in vacuo. EtOAc was added to dilute the residue, filtered and concentrated in vacuo to afford (5,7-difluoroquinolin-6-yl)methanamine (2.70 g, 88%). 1H-NMR (400 MHz, CDCl3) δ ppm 8.93 (d, 1H), 8.38 (d, 1H), 7.59 (d, 1H), 7.43 (m, 1H), 4.12 (s, 2H). LCMS (method B): [MH]+=195.0, tR=0.17 min.

1. temperatureThe solution was heated
2. temperatureat reflux for 3 h
3. temperatureAfter cooling
4. filtrationthe mixture was filtered through celite
5. concentrationThe filtrate was concentrated in vacuo
6. additionEtOAc was added
7. additionto dilute the residue
8. filtrationfiltered
9. concentrationconcentrated in vacuo