反应详情

To a solution (20 ml) of 4-benzylpiperidine (423 mg) and 2,4-dibenzyloxyphenylacetic acid (700 mg) in N,N-dimethylformamide are added triethylamine (0.56 ml) and diethyl cyanophosphate (393 mg) and the mixture is stirred at room temperature for 15 minutes. Water is added and stirring carried out for 10 minutes, followed by extraction of the product with dichloromethane. The dichloromethane layer is washed with water and dried over anhydrous sodium sulfate. The solvent is distilled off. The residue is subjected to purification by silica gel column chromatography. 1-(2,4-Dibenzyloxyphenylacetyl)-4-benzylpiperidine (1.0 g) in the colorless oily form is obtained from a fraction eluted with dichloromethane-ethyl acetate mixture (8:1).

1. stirringstirring
2. waitcarried out for 10 minutes
3. extractionfollowed by extraction of the product with dichloromethane
4. washThe dichloromethane layer is washed with water
5. dry with materialdried over anhydrous sodium sulfate
6. distillationThe solvent is distilled off
7. customThe residue is subjected to purification by silica gel column chromatography