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    Asymmetric catalytic reduction of oxcarbazepine
    3.
    发明授权
    Asymmetric catalytic reduction of oxcarbazepine 有权
    不对称催化还原奥卡西平

    公开(公告)号：EP2319836B1

    公开(公告)日：2015-11-25

    申请号：EP11152286.8

    申请日：2006-04-21

    申请人： Bial-Portela & CA, S.A.

    发明人： Learmonth, David Alexander ,  Grasa, Gabriela Alexandra ,  Zanotti-Gerosa, Antonio

    IPC分类号： C07D223/22

    CPC分类号： C07D223/28 ,  A61K31/55 ,  C07D223/22

    摘要： A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX 2 (L)] 2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R 1 is chosen from C 1-6 alkoxy and C 1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R 1 can be the same or different, and R 2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR 3 R 4 R 5 and formic acid, [R 3 R 4 R 5 NH][OOCH] and optionally formic acid, or [M][OOCH] x and formic acid, wherein R 3 , R 4 and R 5 are C 1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

    Process for the asymmetric hydrogenation of ketones
    6.
    发明公开
    Process for the asymmetric hydrogenation of ketones 有权
    Verfahren zur unfrischen Hydrierung von Ketonen

    公开(公告)号：EP2383261A1

    公开(公告)日：2011-11-02

    申请号：EP10004348.8

    申请日：2010-04-23

    申请人： Archimica GmbH

    发明人： Wisdom, Richard ,  Jung, Jörg ,  Meudt, Andreas

    IPC分类号： C07D223/28

    CPC分类号： C07D223/28 ,  C07B2200/07

    摘要： The invention relates to a process for the asymmetric transfer hydrogenation of a ketone substrate to produce as chiral secondary alcohol with an ee of greater than 85% in which an enantio-enriched chiral catalyst containing ruthenium or rhodium is used with a hydrogen donor and in which an anion exchange resin is used as a base.

    摘要翻译： 本发明涉及一种酮底物的不对称转移氢化方法，以产生ee大于85％的手性仲醇，其中含有钌或铑的富集对en enriched的手性催化剂与氢供体一起使用，其中 使用阴离子交换树脂作为基质。

    METHOD FOR CHEMICAL SYNTHESIS OF OXCARBAZEPINE
    9.
    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。