| 摘要 |
PURPOSE: Provided is a method for preparing cis-4-amino-5-chloro-N-£1-£3-(4-fluorophenoxy)propyl}-3-methoxy-4-piperidinyl|-2-methoxybenzamide which is called cisapride and has stomach- and bowels-motility stimulating activity. The method is environmentally friendly and produces the cisapride with a high yield. CONSTITUTION: A preparation method of cisapride of the formula(1) comprises the reaction of a compound represented by the formula (7) or quaternary ammonium compound represented by the formula (8) with 4-fluorophenol represented by the formula (9) in the presence of a base. Wherein, the reaction temperature is preferably 10-80°C more preferably 50-60°C and one of potassium carbonate, sodium carbonate, sodium hydroxide, potassium hydroxide is used as a base, and alcohol, chloroform, ethyl acetate are used as a solvent. In the formula (7) and (8), X is selected from the group consisting of halogen, hydroxy group, alkylsulfonate and arylsulfonate.
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