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    Process for the synthesis of diricinoleyphosphatidylcholine
    5.
    发明授权
    Process for the synthesis of diricinoleyphosphatidylcholine 失效
    合成二抗磷脂酰胆碱的方法

    公开(公告)号：US06297391B1

    公开(公告)日：2001-10-02

    申请号：US09366744

    申请日：1999-08-04

    申请人： Giampietro Borsotti ,  Ezio Battistel ,  Francesco Cellini ,  Rina Iannacone

    发明人： Giampietro Borsotti ,  Ezio Battistel ,  Francesco Cellini ,  Rina Iannacone

    IPC分类号： C07C5300

    CPC分类号： C12P7/6481 ,  C07F9/10 ,  Y02P20/55

    摘要： Diricinoleylphosphatidylcholine (I) in an optically active form is obtained with good yields and a high purity by means of a process which comprises: a) esterifying the terminal carboxylic group of ricinoleic acid (III) with an alcohol having from 1 to 4 carbon atoms to give the corresponding ester having formula (IV); b) protecting the hydroxylic group of the ester of ricinoleic acid (IV) with a protecting group removable under bland operating conditions and isolating the ester of ricinoleic acid of which the hydroxylic group (V) is protected; c) hydrolyzing the ester of ricinoleic acid of which the hydroxylic group (V) is protected and isolating the ricinoleic acid of which the hydroxylic group (VI) is protected; d) acylating L-&agr;-glycerophosphatidylcholine (II) with an imidazolic or triazolic derivative of the compound having formula (VI) and isolating the diricinoleylphosphatidylcholine of which the hydroxylic group (VII) is protected; e) removing the protecting group from the hydroxylic group of the compound having formula (VII); and finally f) recovering and purifying the compound having formula (I) by means of chromatography.

    摘要翻译： 通过以下方法获得具有光学活性形式的二亚油酰基磷脂酰胆碱（I），具有良好的收率和高纯度，该方法包括：a）用具有1至4个碳原子的醇将蓖麻油酸（III）的末端羧基酯化至 得到具有式（IV）的相应酯; b）用温和的操作条件下可除去的保护基保护蓖麻油酸（IV）的酯的羟基，并将其中羟基（Ⅴ）的蓖麻油酸酯 保护; c）水解羟基（V）被保护的蓖麻油酸酯，并分离保护羟基（Ⅵ）的蓖麻油酸; d）用咪唑单体酰化L-α-甘油磷脂酰胆碱（II） 或具有式（Ⅵ）的化合物的三唑衍生物，并分离保护羟基（Ⅶ）的二亚油酰基磷脂酰胆碱; e）从羟基中除去保护基 具有式（VII）的化合物的式 最后通过色谱法回收和纯化具有式（I）的化合物。