Method for the Preparation of Fentanyl
    7.
    发明申请
    Method for the Preparation of Fentanyl 有权
    芬太尼制备方法

    公开(公告)号:US20110021781A1

    公开(公告)日:2011-01-27

    申请号:US12922906

    申请日:2009-03-09

    CPC classification number: C07D211/58

    Abstract: The invention provides a method for the preparation of fentanyl comprising: (a) reacting 4-piperidone hydrochloride (NPP) with aniline in presence of reducing environment to produce 4-anilinopiperidine (4-ANPP), (b) reacting the 4-ANPP as obtained from step (a) with phenethyl halide under reflux conditions in highly alkaline medium to give 4-anilino-N-phenethylpiperidine, and (c) converting the 4-anilino-N-phenethylpiperidine to fentanyl by reacting with propionyl chloride in presence of halogenated hydrocarbons, then isolating fentanyl by solvent extraction and purifying by crystallization from petroleum ether at a temperature ranging from 60-80° C.

    Abstract translation: 本发明提供了一种制备芬太尼的方法,包括:(a)在还原环境存在下使4-哌啶酮盐酸盐(NPP)与苯胺反应以产生4-苯胺基哌啶(4-ANPP),(b)使4-ANPP作为 在高碱性介质中在回流条件下用步骤(a)得到步骤(a),得到4-苯胺基-N-苯乙基哌啶,和(c)通过与丙酰氯在卤化物存在下反应将4-苯胺基-N-苯乙基哌啶转化成芬太尼 烃,然后通过溶剂萃取分离芬太尼,并在60-80℃的温度下从石油醚中结晶纯化。

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