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    METHOD FOR CHEMICAL SYNTHESIS OF OXCARBAZEPINE
    2.
    发明公开
    METHOD FOR CHEMICAL SYNTHESIS OF OXCARBAZEPINE 审中-公开
    VERFAHREN ZUR CHEMISCHEN SYNTHESE VON OXCARBAZEPIN

    公开(公告)号：EP2311812A1

    公开(公告)日：2011-04-20

    申请号：EP09771966.0

    申请日：2009-06-30

    申请人： Zhejiang University Of Technology ,  Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

    发明人： SU, Weike ,  LI, Jianjun ,  JIANG, Zulin ,  XU, Jiankang ,  SONG, Gang ,  CHE, Daqing

    IPC分类号： C07D223/22 ,  A61P25/08

    CPC分类号： C07D223/26 ,  C07D223/28

    摘要： Method for chemical synthesis of oxcarbazepine comprises adding 5-cyano-10-nitro-5H-dibenz[b,f]azepine of formula III, Raney nickel catalyst, and organic solvent into a reactor, adding hydrogen at 2-20A, controlling the temperature to 40-120°C and carrying out reduction reaction, filtering after reacting completely, hydrolyzing the filtrate by adding 20-36.5 mass% hydrochloric acid, concentrating and cooling crystallizing the reaction solution, and obtaining the oxcarbazepion. The method has advantages of advanced process, simple and safe operation, and high product purity and yield, which is suitable for commercial production.

    摘要翻译： 化学合成奥卡西平的方法包括将式III的5-氰基-10-硝基-5H-二苯并[b，f]吖庚因，阮内镍催化剂和有机溶剂加入反应器中，加入2-20A的氢气，控制温度 至40-120℃，进行还原反应，完全反应后过滤，加入20-36.5质量％盐酸水解滤液，浓缩并冷却反应溶液结晶，得到奥卡泽菌素。 该方法工艺先进，操作简单安全，产品纯度高，产量高，适合商业生产。

    INTERMEDIATE OF EDOXABAN TOSYLATE AND PREPARATION METHOD THEREFOR
    3.
    发明公开
    INTERMEDIATE OF EDOXABAN TOSYLATE AND PREPARATION METHOD THEREFOR 审中-公开

    公开(公告)号：EP4450508A1

    公开(公告)日：2024-10-23

    申请号：EP21967736.6

    申请日：2021-12-17

    申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

    发明人： MEI, Yijiang ,  LIU, Shengmin ,  LI, Yonggang ,  FAN, Jinmin ,  HU, Kai ,  GAO, Shizhao

    IPC分类号： C07D513/04 ,  C07D211/74

    摘要： Disclosed are an intermediate of edoxaban tosylate and a preparation method therefor, having the advantages that the preparation process is simple, reaction conditions are mild, the cost is low, and raw materials are easily to be obtained. The method comprises the synthesis steps of: substitution reaction, thiolation reaction, cyclization reaction, esterification reaction with alcohol to obtain a compound represented by formula (V), and then reacting to obtain a compound represented by formula (VI), or directly reacting the compound represented by formula (IV) under the effect of alcohol and acid, to obtain the compound represented by formula (VI), and subjecting the compound represented by formula (VI) to alkali hydrolysis and acid neutralization to obtain a compound represented by formula (VII). The reaction formula is as follows:

    CHIRAL SPIRO PHOSPHORUS-NITROGEN-SULPHUR TRIDENTATE LIGAND, AND PREPARATION METHOD AND APPLICATION THEREOF
    4.
    发明公开
    CHIRAL SPIRO PHOSPHORUS-NITROGEN-SULPHUR TRIDENTATE LIGAND, AND PREPARATION METHOD AND APPLICATION THEREOF 审中-公开
    手性螺旋磷 - 氮 - 硫 - 三齿配体及其制备方法和应用

    公开(公告)号：EP3296302A1

    公开(公告)日：2018-03-21

    申请号：EP16795647.3

    申请日：2016-01-26

    申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

    发明人： ZHOU, Qilin ,  XIE, Jianhua ,  BAO, Denghui ,  WANG, Lixin

    IPC分类号： C07F9/50 ,  B01J31/24 ,  C07B41/02 ,  C07C67/31 ,  C07C69/675 ,  C07C69/708 ,  C07C269/06 ,  C07C271/22 ,  C07C231/12 ,  C07C235/06 ,  C07C29/145

    CPC分类号： C07F9/5022 ,  B01J31/189 ,  B01J31/226 ,  B01J31/249 ,  B01J37/04 ,  B01J2231/643 ,  B01J2531/0241 ,  B01J2531/827 ,  C07B53/00 ,  C07C29/145 ,  C07C29/149 ,  C07C67/31 ,  C07C69/675 ,  C07C69/708 ,  C07C231/12 ,  C07C231/18 ,  C07C235/06 ,  C07C269/06 ,  C07C271/22 ,  C07F9/5054 ,  C07F9/655363 ,  C07F15/0033

    摘要： The present invention relates to a chiral spiro phosphine-nitrogen-sulfur (P-N-S) tridentate ligand, preparation method and application thereof. The P-N-S tridentate ligand is a compound represented by Formula I or Formula II, their racemates, optical isomers, or catalytically acceptable salts thereof. The ligand has a primary structure skeleton characterized as a chiral spiro indan skeleton structure with a thio group. The chiral spiro phosphine-nitrogen-sulfur tridentate ligand can be synthesized by reacting racemic or optical active compound 7-diary/alkyl phosphine-7'-amino-1, 1'-spiro-dihydro- indene compound having a spiro-dihydro-indene skeleton as the starting material. The chiral spiro P-N-S tridentate ligand being complex with transition metal salt can be used in an asymmetric catalytic hydrogenation reaction for catalyzing carbonyl compound. In particular, in asymmetric hydrogenation reaction process, being complex with iridium for catalyzing β-alkyl-β-keto ester can obtain a high catalytic activity (a catalyst amount of 0.0002% mol) and high enantioselectivity (up to 99.9% ee) result. So the present invention has a practical value for industrial and commercial production.

    摘要翻译： 手性螺环膦 - 氮 - 硫（P-N-S）三齿配体及其制备方法和应用技术领域本发明涉及手性螺环膦 - 氮 - 硫（P-N-S）三齿配体及其制备方法和应用。 P-N-S三齿配体是由式I或式II表示的化合物，其外消旋体，旋光异构体或其催化可接受的盐。 该配体具有一级结构骨架，其特征在于具有硫基的手性螺茚骨架结构。 手性螺环膦 - 氮 - 硫 - 三齿配体可通过使具有螺 - 二氢 - 茚的外消旋或光学活性化合物7-二芳基/烷基膦-7'-氨基-1,1'-螺 - 二氢茚化合物 骨架作为起始材料。 与过渡金属盐络合的手性螺环P-N-S三齿配体可用于催化羰基化合物的不对称催化氢化反应。 特别是在不对称氢化反应过程中，与铱配合催化β-烷基-β-酮酯可获得高催化活性（催化剂用量为0.0002摩尔％）和高对映选择性（高达99.9％ee）。 所以本发明对于工业和商业生产具有实际价值。

    METHOD FOR ASYMMETRICALLY CATALYZED SYNTHESIS OF NITROPYRAZOLE AMIDE COMPOUND
    6.
    发明公开
    METHOD FOR ASYMMETRICALLY CATALYZED SYNTHESIS OF NITROPYRAZOLE AMIDE COMPOUND 审中-公开
    非对称催化合成硝基吡唑酰胺化合物的方法

    公开(公告)号：EP3199525A1

    公开(公告)日：2017-08-02

    申请号：EP15844037.0

    申请日：2015-06-12

    申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

    发明人： FENG, Xiaoming ,  YAO, Qian ,  LIU, Xiaohua ,  LIN, Lili ,  ZHANG, Yuheng

    IPC分类号： C07D231/12 ,  C07D231/16 ,  C07D333/24 ,  C07C205/53 ,  C07C201/12 ,  C07D207/267 ,  C07D307/54

    CPC分类号： C07D211/88 ,  C07C201/12 ,  C07C205/53 ,  C07D207/267 ,  C07D231/12 ,  C07D231/16 ,  C07D405/06 ,  C07D409/06

    摘要： An asymmetrically catalyzed synthesis method of a γ-nitropyrazole amide compound is provided, wherein in the reaction that a nitroalkane and an α,β-unsaturated pyrazole amide are employed as raw materials, a complex formed by a chiral amine oxide with a rare earth metal compound is served as a catalyst, a 4 Å molecular sieve is served as an additive, after the reaction finished, to obtain a γ-nitropyrazole amide compound. The reaction has a yield more than 99% and an enantiomeric excess more than 99% ee. The catalytic system not only has the advantages of simple operation, mild reaction conditions, requiring no acid/base additives, convenient product purification, high yield and enatioselectivity, compliance with green atomic economy, and promising prospects for industrial application, but also allows the obtained γ-nitropyrazole amide compound to undergo some simple chemical conversions to produce some molecules having physiological activities.

    摘要翻译： 本发明提供一种γ-硝基吡唑酰胺化合物的不对称催化合成方法，其中以硝基烷烃和α，β-不饱和吡唑酰胺为原料的反应中，由手性氧化胺与稀土金属形成的配合物 化合物用作催化剂，在反应完成后用4分子筛作为添加剂，得到γ-硝基吡唑酰胺化合物。 该反应的收率超过99％，对映体过量超过99％ee。 该催化体系不仅具有操作简单，反应条件温和，不需要酸碱添加剂，产品纯化方便，产率高，选择性好，符合绿色原子经济，具有广阔的工业应用前景等优点， γ-硝基吡唑酰胺化合物进行一些简单的化学转化以产生一些具有生理活性的分子。

    A METHOD FOR PREPARING 5H-CYANO-IMIDO STILBENE
    9.
    发明公开
    A METHOD FOR PREPARING 5H-CYANO-IMIDO STILBENE 有权
    一种制备5H-氰基咪唑的方法

    公开(公告)号：EP2311813A1

    公开(公告)日：2011-04-20

    申请号：EP09771967.8

    申请日：2009-06-30

    申请人： Zhejiang University Of Technology ,  Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

    发明人： SU, Weike ,  SHI, Xiangjun ,  CHE, Daqing ,  LIN, Jinrong ,  HU, Kai

    IPC分类号： C07D223/26

    CPC分类号： C07D223/26

    摘要： A method for preparing 5-cyano-5H-dibenz[b,f]azepine, comprises: reacting carbamazepine of formula (II) used as dehydrating agent with bis(trichloromethyl)carbonate of formula (III) in organic solvent for 1-30 hours at 20-150°C, and obtaining 5-cyano-5H-dibenz[b,f]azepine (I) after the post-treatment of the reaction solution. The scheme is shown as below.

    摘要翻译： 制备5-氰基-5H-二苯并[b，f]氮杂的方法包括：将用作脱水剂的式（II）的卡马西平与式（III）的双（三氯甲基）碳酸酯在有机溶剂中反应1-30小时 在20-150℃下反应，并且在反应溶液的后处理之后获得5-氰基-5H-二苯并[b，f]氮杂（I）。 该方案如下所示。