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    METHOD FOR ENZYMATIC PREPARATION OF FLUDARABINE PHOSPHATE
    4.
    发明公开
    METHOD FOR ENZYMATIC PREPARATION OF FLUDARABINE PHOSPHATE 审中-公开

    公开(公告)号：EP3406729A1

    公开(公告)日：2018-11-28

    申请号：EP16885588.0

    申请日：2016-01-20

    申请人： Zhejiang Hisun Pharmaceutical Co., Ltd.

    发明人： FU, Dejin ,  YANG, Yong ,  YAN, Wei ,  WEN, Weijiang ,  GU, Xiande ,  CHEN, Hua ,  MA, Xiaojun ,  ZHANG, Ling ,  WANG, Kaijun

    IPC分类号： C12P19/30 ,  C12P19/32 ,  C07H19/20

    CPC分类号： C07H19/20 ,  C12P19/30 ,  C12P19/32

    摘要： A method for enzymatic preparation of fludarabine phosphate, comprising reaction of fludarabine with a high-energy phosphate compound under the action of deoxyribonucleic acid kinase. According to said method, acetate kinase and acetyl phosphate free acid or acetyl phosphate are also added. The technical problems present in the existing processes are successfully addressed by employing the enzymatic process to prepare the fludarabine phosphate. The usage of the high-energy phosphate compound is reduced by means of adding acetate kinase to recycle and regenerate a small amount of the high-energy phosphate compound, thereby reducing the generation of by-products having similar structures to the fludarabine phosphate, enhancing the operation convenience of purification steps in the industrial production of the fludarabine phosphate. The process is environment friendly, the reaction conditions are moderate, the cost is low, and the yield and the purity of the product obtained are high.

    PREPARATION METHOD FOR PRAZIQUANTEL AND INTERMEDIATE COMPOUNDS THEREOF
    6.
    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 STALLIMYCIN
    7.
    发明公开
    METHOD FOR PREPARING STALLIMYCIN 审中-公开
    制备司米卡利的方法

    公开(公告)号：EP3239300A1

    公开(公告)日：2017-11-01

    申请号：EP15871790.0

    申请日：2015-11-10

    申请人： Zhejiang Hisun Pharmaceutical Co., Ltd.

    发明人： JIANG, Shichun ,  JIANG, Huan

    IPC分类号： C12P17/16 ,  C12R1/465

    CPC分类号： C12P17/16 ,  C12R1/465

    摘要： Provided is a method for preparing stallimycin. The method comprises: fermenting streptomyces in a fermentation medium comprising a carbon source, a nitrogen source and 3-hydroxy-4-aminobutyric acid, and adding vegetable oil into the fermentation medium during the fermentation.

    摘要翻译： 提供了一种制备维拉霉素的方法。 该方法包括：在包含碳源，氮源和3-羟基-4-氨基丁酸的发酵培养基中发酵链霉菌，并在发酵过程中将植物油加入发酵培养基中。