反应详情

To a solution of lithium aluminium hydride (0.9 g) in anhydrous tetrahydrofuran (160 ml) is added 2-(1-benzyl-4-piperidinylamino)-6-fluorobenzoic acid (8.0 g) and the mixture is refluxed for 1 hour. After cooling, the reaction solution is poured into ice-water and then extracted with dichloromethane. The solvent is concentrated and to the resulting residue is added diethyl ether/n-hexane. The precipitated crystal is collected by filtration to give N-(1-benzyl-4-piperidinyl)-2-hydroxymethyl-3-fluoroaniline (4.6 g) as light yellow powders, m.p.: 167°-170° C.

1. temperaturethe mixture is refluxed for 1 hour
2. temperatureAfter cooling
3. extractionextracted with dichloromethane
4. concentrationThe solvent is concentrated and to the resulting residue
5. additionis added diethyl ether/n-hexane
6. filtrationThe precipitated crystal is collected by filtration