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    A METHOD OF PREPARING MEMANTINE HYDROCHLORIDE
    1.
    发明公开
    A METHOD OF PREPARING MEMANTINE HYDROCHLORIDE 有权
    用于生产盐酸美金刚

    公开(公告)号：EP1674446A4

    公开(公告)日：2009-09-09

    申请号：EP03785457

    申请日：2003-12-19

    申请人： SHANGHAI INST PHARM INDUSTRY ,  ZHEJIANG KANGYU PHARMACEUTICAL

    发明人： ZHANG FULI ,  HU MENG ,  ZHAO LIZHI ,  GE MENGYA

    IPC分类号： C07C211/38 ,  A61P25/28 ,  C07C209/08

    CPC分类号： C07C209/08 ,  C07C211/38

    摘要： A new method of preparing memantine hydrochloride, comprises the following steps: reacting 1-bromo-3, 5-dimethyl adamantane and urea/formic acid with formic acid also acting as the solvent; hydrolysising with aqueous inorganic acid; alkalifying, extracting and acidifying with hydrochloric acid; finally collecting target compound. The method uses cheaper raw materials and conducts in homogeneous phase under mild conditions. It can reach high yield and good product purity, and be suitable for macrochemistry. The purity of crude product is 99.0%, and reaches 99.98% after first recrystallization, yield: 69.5%, bp: 332ºC (DSC).

    PREPARATION METHOD FOR RIVASTIGMINE, INTERMEDIATES THEREOF, AND PREPARATION METHOD FOR SAID INTERMEDIATES
    3.
    发明公开
    PREPARATION METHOD FOR RIVASTIGMINE, INTERMEDIATES THEREOF, AND PREPARATION METHOD FOR SAID INTERMEDIATES 有权
    工艺用于其及其制造方法利斯的明中间体中间体

    公开(公告)号：EP2711354A4

    公开(公告)日：2015-05-06

    申请号：EP12785792

    申请日：2012-05-16

    申请人： ZHEJIANG HISUN PHARM CO LTD ,  SHANGHAI INST PHARM INDUSTRY

    发明人： ZHANG FULI ,  YANG ZHEZHOU ,  YANG CHUNBO ,  CHEN DAOXIN ,  YANG ZHIQING ,  SUN RENTONG ,  BAI HUA

    IPC分类号： C07C211/27 ,  A61K31/27 ,  A61P25/28 ,  C07C269/06 ,  C07C271/44

    CPC分类号： C07C271/44 ,  C07B2200/07 ,  C07C215/66 ,  C07C217/58 ,  C07C269/04 ,  C07C269/06 ,  C07C309/04

    摘要： The present invention provides the preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate (formula X compound), the preparation methods for its intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium(formula VI compound), (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium(formula VIII compound) and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium (formula IX compound), as well as the method for using above mentioned formula IX compound to prepare rivastigmine which can be used for the treatment of Alzheimer's disease. The preparation method for rivastigmine has a reasonable synthetic design with convenient source of raw materials and high total yield, and the product resulted has high chemical and optical purity, which makes it easy for large-scale. industrial production.

    摘要翻译： 本发明提供了用于制备方法（S）-3-（1-（二甲基氨基）乙基）苯基乙基（甲基）氨基甲酸叔丁酯（式X的化合物），其中间体的制备方法（S）-1-（3-甲氧基苯基 基）-N，N-二甲基-N - （（S）-1-苯乙基）乙铵（式VI化合物），（S）-1-（3-羟基苯基）-N，N-二甲基-N - （（S） -1-苯乙基）乙铵（（式VIII化合物）和（S）-1-（3-乙基（甲基）氨基甲酰氧基）苯基）-N，N-二甲基-N - （（S）-1-苯乙基）乙铵（ 式IX化合物），以及用于使用上述式IX化合物，以制备卡巴拉汀哪些可用于阿尔茨海默氏病的治疗方法。 对于利凡斯的明的制备方法具有与原料及高总收率的方便来源合理设计合成的，并且产品已经导致高的化学和光学纯度，这使得它易于进行大规模。 工业生产。