| 摘要 |
PURPOSE: A manufacturing method of piperidine derivatives and pharmaceutically acceptable salt thereof is provided, which simplifies the process and is cost effective by using cheap raw materials. CONSTITUTION: Piperidine derivative of formula (1) is prepared by reacting compound of formula (2) and compound of formula (3). Wherein, R1 and R2 are independently hydrogen, alkyl groups of linear chain or branched chain having 1-6 carbons or selected from cycloalkyl group having 3-6 carbons; M is alkali metal or halogenated metal. A preparation method of ethyl 4-(4-hydroxypiperidino)butanoate comprises the steps of: adding 5.0g of 4-hydroxypiperidine, 0.9g of sodium carbonate, 80mg of potassium iodine, 5.0g of ethyl chlrobutylate to 50ml of ethyl acetate, circulation-shaking for 20hrs; cooling to room temperature, filtering, washing the organic layer twice with water, and extracting the water layer with ethylacetate; adding the organic layer, drying with magnesium sulfate; filtering, concentrating under decompression to get 8.5g of objective material.
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