反应详情

Hydrazine (10 ml) was added to a solution of 2-[1-(3,5-dichloro-2-hydroxy-benzyl)-4-fluoro-piperidin-4-ylmethyl]-isoindole-1,3-dione (20.7 g) in ethanol (600 ml). The obtained solution was stirred for 5 hours while heating to reflux, and then subjected to heated filtration. The filtrate was concentrated, water was added to the residue, and then extraction with dichloromethane was followed by concentration. The obtained residue was recrystallized from isopropyl ether-pentane to obtain 2-(4-aminomethyl-4-fluoro-piperidin-1-ylmethyl)-4,6-dichlorophenol.

1. temperaturewhile heating
2. temperatureto reflux
3. temperatureto heated
4. filtrationfiltration
5. concentrationThe filtrate was concentrated
6. additionwater was added to the residue
7. extractionextraction with dichloromethane
8. concentrationwas followed by concentration
9. customThe obtained residue was recrystallized from isopropyl ether-pentane