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    PREPARATION METHOD FOR PRAZIQUANTEL AND INTERMEDIATE COMPOUNDS THEREOF
    1.
    发明公开
    PREPARATION METHOD FOR PRAZIQUANTEL AND INTERMEDIATE COMPOUNDS THEREOF 审中-公开
    吡喹酮及其中间体化合物的制备方法

    公开(公告)号：EP3257852A1

    公开(公告)日：2017-12-20

    申请号：EP15881512.6

    申请日：2015-02-12

    申请人： Zhejiang Hisun Pharmaceutical Co., Ltd. ,  Shanghai Institute Of Pharmaceutical Industry

    发明人： ZHANG, Fuli ,  YANG, Zhezhou ,  BAO, Rusheng ,  XU, Weiwei ,  BAI, Hua

    IPC分类号： C07D471/04 ,  A61K31/4985 ,  A61P33/00 ,  A61P33/12

    摘要： Disclosed are a preparation method for praziquantel and intermediates thereof. The method comprises: a target product praziquantel is obtained by using β-phenethylamine as an initial raw material through the condensation reaction with chloroacetyl chloride, the substitution reaction with ethanolamine, and the acylation reaction with cyclohexanecarbonyl chloride, and then followed by the oxidation reaction and the cyclization reaction. Also disclosed are two key intermediates, namely, a formula IV compound and a formula V compound for preparing the praziquantel. The preparation method is reasonable and simple in technological design, moderate in reaction conditions, economical and environment-friendly; raw materials are inexpensive and easy to get, the key intermediates are easy to prepare, the total reaction yield is high (≥ 60%), and the purity of the obtained target product formula I compound praziquantel is high (the HPLC determined purity ≥ 99.8%), so that the industrialized mass production is easy to realize.

    摘要翻译： 公开了一种吡喹酮及其中间体的制备方法。 该方法包括：以β-苯乙胺为起始原料，经与氯乙酰氯缩合反应，与乙醇胺发生取代反应，与环己烷甲酰氯酰化反应，然后进行氧化反应，得到目标产物吡喹酮， 环化反应。 还公开了两种关键中间体，即用于制备吡喹酮的式IV化合物和式V化合物。 本发明工艺设计合理简单，反应条件温和，经济环保; 原料廉价易得，关键中间体易于制备，总反应收率高（≥60％），且所得目标产物式I化合物吡喹酮纯度高（HPLC测定纯度≥99.8 ％），因此工业化大规模生产很容易实现。

    4-BENZYL-1-PHENETHYL-PIPERAZINE-2,6-DIONE PREPARATION METHOD, AND INTERMEDIATE AND PREPARATION METHOD THEREOF
    5.
    发明公开
    4-BENZYL-1-PHENETHYL-PIPERAZINE-2,6-DIONE PREPARATION METHOD, AND INTERMEDIATE AND PREPARATION METHOD THEREOF 有权
    METHOD FOR PRODUCING 4-苄基-1-苯乙基 - 哌嗪-2,6-二酮及其中间体及其制造方法

    公开(公告)号：EP3015455A1

    公开(公告)日：2016-05-04

    申请号：EP14817699.3

    申请日：2014-06-23

    申请人： Zhejiang Hisun Pharmaceutical Co. Ltd. ,  Shanghai Institute Of Pharmaceutical Industry

    发明人： ZHANG, Fuli ,  YANG, Zhezhou ,  BAO, Rusheng ,  QIU, Pengcheng ,  JIN, Linyong ,  PAN, Hu ,  PAN, Linyu ,  JIANG, Dongming ,  XU, Weiwei

    IPC分类号： C07C237/06 ,  C07C231/02 ,  C07D241/08 ,  C07D471/04

    CPC分类号： C07C237/06 ,  C07C231/02 ,  C07C231/10 ,  C07D241/08 ,  C07D471/04

    摘要： The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity.

    摘要翻译： 本发明提供的一个关键新的中间4-苄基-1-苯乙基 - 哌嗪-2,6-二酮（式IV化合物），其药学上可接受的盐和它们的制备方法（式III的化合物）。 此外，本发明盘松的方法用于从式III化合物制备4-苄基-1-苯乙基 - 哌嗪-2,6-二酮（式IV化合物），所述方法克服了当前的式IV化合物的制备方法的短缺憾，：如 低生产量，低纯度，高能耗，成本高，而且无法实现工业化生产，并提供了式IV化合物的制备方法，其全部是简单，经济，环境友好且易于生产工业上; 该方法的反应溶剂容易回收，并且该方法可产生在高生产率和高纯度的式IV化合物。