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。

公开(公告)号：EP2311813B1

公开(公告)日：2013-09-11

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

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。

公开(公告)号：EP2801567A1

公开(公告)日：2014-11-12

申请号：EP12862614.0

申请日：2012-07-27

申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

发明人： ZHANG, Bin ,  HU, Xiaowei ,  YAN, Pucha ,  ZHANG, Xianyi ,  GAO, Hongjun ,  LI, Yuanqiang ,  CHE, Daqing

IPC分类号： C07D209/08 ,  C07D209/04 ,  C07D209/02 ,  C07F7/18 ,  C07F7/02 ,  C07F7/00

CPC分类号： C07D209/08 ,  C07F7/00 ,  C07F7/02 ,  C07F7/18 ,  C07F9/65397 ,  Y02P20/55

摘要： Disclosed are a silodosin intermediate and a preparation method thereof. The silodosin intermediate has the structure shown by the formula (A). X is hydrogen or bromide and R 1 is hydrogen. The formyl group may be a group having the structure shown by the formula I. R 7 is an carboxyl-protecting group, and R 2 is 3-hydroxypropyl or a group having the structure shown by the formula II. W is a hydroxyl-protecting group. A compound of the formula (A) according to the present invention may further be used for preparing a compound having the structure shown by the formula (D). By means of the intermediate and the preparation method therefor provided by the present invention, high-purity optically pure silodosin can be obtained, and the optical purity is above 99%.

摘要翻译： 公开了一种西洛多辛中间体及其制备方法。 西洛多辛中间体具有式（A）所示的结构。 X是氢或溴，R1是氢。 甲酰基可以是具有式I所示结构的基团。R 7是羧基保护基，R 2是3-羟基丙基或具有式II所示结构的基团。 W是羟基保护基。 根据本发明的式（A）化合物还可以用于制备具有式（D）所示结构的化合物。 通过本发明提供的中间体及其制备方法，可以得到高纯度的光学纯的西洛多辛，光学纯度在99％以上。

公开(公告)号：EP3015456A1

公开(公告)日：2016-05-04

申请号：EP14816731.5

申请日：2014-06-23

申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

发明人： ZHANG, Bin ,  LI, Yuanqiang ,  CHE, Daqing ,  QIAN, Lingfeng ,  ZHU, Guoliang ,  YE, Wenfa

IPC分类号： C07D207/22 ,  C07D207/46 ,  C07D207/16

CPC分类号： C07D207/22 ,  C07D207/16 ,  Y02P20/55

摘要： The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R 1 or R2, R1 is C1-C6 an alkyl, benzyl, p-methoxybenzyl, or p-nitrobenzyl group, and R2 is hydrogen; R3 is a protecting group of the carboxyl group; and P1 is a protecting group on nitrogen.

摘要翻译： 本发明涉及医药合成领域，特别涉及吡咯烷-2-羧酸衍生物的制备方法。 本发明采用以下技术方案：提供具有式（E）结构的化合物，其中R为R 1或R 2，R 1为C 1 -C 6烷基，苄基，对甲氧基苄基或对硝基苄基， R2是氢; R3是羧基的保护基; P1是氮的保护基。