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    Crystalline carbapenem compound and produced method thereof
    3.
    发明公开
    Crystalline carbapenem compound and produced method thereof 审中-公开
    Kristalline Carbapenem-Verbindung und Herstellungsverfahrendafür

    公开(公告)号：EP2098525A1

    公开(公告)日：2009-09-09

    申请号：EP08101985.3

    申请日：2008-02-26

    申请人： Savior Lifetec Corporation

    发明人： Tseng, Wei-Hong ,  Su, Yu-Lun ,  Yu, Chiung-Yi

    IPC分类号： C07D477/20 ,  A61K31/4025 ,  A61P31/04

    CPC分类号： C07D477/20

    摘要： The present invention relates to a crystalline carbapenem compound and produced method thereof. The crystalline carbapenem compound of the present invention is crystalline (4 R ,5 S ,6 S )-3-[[(3 S ,5 S )-5-[(dimethylamino)carbonyl]-3-pyrrolidinyl]thio]-6-[(1 R )-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0] hept-2-ene-2-carboxylic acid and it is characterized by an X-ray powder diffraction pattern of Fig. 2 . The crystalline carbapenem compound of the present invention is a new crystalline form and is useful as an antibiotic agent. Furthermore, the crystalline carbapenem compound of the present invention is much more stable than carbapenem compound in a non-crystalline form. Hence, the crystalline carbapenem compound of the present invention is suitable for storage.

    摘要翻译： 本发明涉及结晶碳青霉烯化合物及其制备方法。 本发明的结晶碳青霉烯化合物是结晶（4R，5S，6S）-3 - [[（3S，5S）-5 - [（二甲基氨基）羰基] -3-吡咯烷基]硫基] -6 - [（1R）-1-羟乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸，其特征在于X射线粉末衍射图 的图。 2。 本发明的结晶碳青霉烯化合物是新的结晶形式，可用作抗生素。 此外，本发明的结晶碳青霉烯化合物比非结晶形式的碳青霉烯化合物稳定得多。 因此，本发明的结晶碳青霉烯化合物适合贮存。

    Method for manufacturing stereoselective preparation of 4-bma using a chiral auxiliary and chiral auxiliary
    5.
    发明公开
    Method for manufacturing stereoselective preparation of 4-bma using a chiral auxiliary and chiral auxiliary 审中-公开
    一种用于使用手性辅助和手性助剂制备4-BMA的立体选择性制备方法

    公开(公告)号：EP2345645A1

    公开(公告)日：2011-07-20

    申请号：EP09180507.7

    申请日：2009-12-22

    申请人： Savior Lifetec Corporation

    发明人： Tseng, Wei-Hong ,  Chuang, Shiuan-Ting ,  Hung, Zun-Yuan ,  Wu, Ching-I

    IPC分类号： C07D263/20 ,  C07D413/06

    CPC分类号： C07D413/06 ,  C07D263/20

    摘要： The present invention relates to a process for preparing (3R,4S)-3- [[[R]-1 ' -t-butyldimethylsilyloxy ]ethyl]-4-[(R)-1 "-carboxyethyl]-2-azetidinone (beta- methylazetidin-2-one; 4-BMA), a key intermediate for the synthesis of carbapenem and penem antibiotics. Specifically, the present invention relates to a process comprising first, the preparation of a chiral auxiliary from cheap L-Phenylalaninol, and then the preparation of 4-BMA in high yield and high selectivity, under industrially mild condition.

    摘要翻译： 本发明涉及一种用于制备（3R，4S）-3 - [[[R] -1 - 叔丁基二甲硅氧基]乙基] -4 - [（R）-1“羧乙基] -2-氮杂环丁酮（ 的β-甲基氮杂环丁烷-2-酮，4-BMA），对碳青霉烯类和青霉烯抗生素的合成中的关键中间体具体地，本发明涉及包括第一过程，从廉价的L-苯丙手性助剂，和制备。 然后4-BMA的以高产率和高选择性制备方法，在工业上温和条件下。