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    PREPARATION METHOD FOR PRAZIQUANTEL AND INTERMEDIATE COMPOUNDS THEREOF
    2.
    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。

    METHOD FOR PREPARING RIVAROXABAN INTERMEDIATE
    4.
    发明公开
    METHOD FOR PREPARING RIVAROXABAN INTERMEDIATE 有权
    制备RIVAROXABAN中间体的方法

    公开(公告)号：EP2837628A1

    公开(公告)日：2015-02-18

    申请号：EP13751142.4

    申请日：2013-02-22

    申请人： China National Medicines Guorui Pharmaceutical Co., Ltd. ,  Shanghai Institute Of Pharmaceutical Industry

    发明人： ZHANG, Fuli ,  LIANG, Bin ,  YANG, Chunbo ,  LIU, Chonghao ,  GAO, Yang ,  WANG, Jian ,  JIANG, Min

    IPC分类号： C07D413/10 ,  C07D413/14

    CPC分类号： C07D413/10 ,  C07D413/14 ,  Y02P20/55

    摘要： Disclosed is a method for preparing a Rivaroxaban intermediate I, comprising the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and ( S )-epoxy compound (III), the reaction temperature ranging from 20° C to 60° C, where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.

    摘要翻译： 公开了一种制备利伐沙班中间体I的方法，包括以下步骤：在非质子溶剂中，在路易斯酸的作用下，对4-（4-苯基异氰酸酯）吗啉-3-酮（II）进行环化反应， 和（S） - 环氧化合物（III），反应温度为20℃至60℃，其中R为氨基被氨基保护基取代。 本发明的制备方法条件温和，工艺简单，成本低，效率高; 该产品易于净化，该方法适用于工业生产。

    PROCESS FOR THE PREPARATION OF 4-(1-HYDROXY-1-METHYLETHYL)-2-PROPYL-IMIDAZOLE-5-CARBOXYLATES
    9.
    发明公开
    PROCESS FOR THE PREPARATION OF 4-(1-HYDROXY-1-METHYLETHYL)-2-PROPYL-IMIDAZOLE-5-CARBOXYLATES 有权
    VERFAHREN ZUR HERSTELLUNG VON 4-（1-羟基-1-甲基乙基）-2-丙氧基咪唑-5-羧酸酯

    公开(公告)号：EP2374799A1

    公开(公告)日：2011-10-12

    申请号：EP08878075.4

    申请日：2008-11-17

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

    发明人： ZHANG, Fuli ,  WU, Taizhi ,  XIE, Meihua

    IPC分类号： C07D233/90 ,  C07D491/048

    CPC分类号： C07D233/90 ,  C07D491/048

    摘要： The present invention discloses a process for obtaining 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylate (formula I) by the reaction of 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole (formula II), or its hydrolysis product, or its ring-opening product, with alcohol under appropriate catalytic conditions. Furthermore, the present invention also provides a process for obtaining high purity 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole (formula II), therefore purified compound of formula I can be produced. Producing of olmesartan medoxomil at high purity is assured by said processes. R in formula I is selected from C 1 -C 6 alkyl.

    摘要翻译： 本发明公开了4-（1-羟基-1-甲基乙基）-2-丙基 - 咪唑-5-羧酸酯（式I）的方法，通过4,4-二甲基-2-丙基-4,6 - 二氢呋喃并[3,4-d]咪唑（式II）或其水解产物或其开环产物与醇在合适的催化条件下反应。 此外，本发明还提供了获得高纯度4,4-二甲基-2-丙基-4,6-二氢呋喃并[3,4-d]咪唑（式II）的方法，因此可以制备纯化的式I化合物 。 通过所述方法可以保证高纯度的奥美沙坦酯的生产。 式I中的R选自C 1 -C 6烷基。