SYNTHESIS OF DECITABINE
    41.
    发明公开
    SYNTHESIS OF DECITABINE 审中-公开
    合成丹皮酚

    公开(公告)号:EP2483250A1

    公开(公告)日:2012-08-08

    申请号:EP10820956.0

    申请日:2010-02-04

    CPC classification number: C07H13/08 C07H19/12

    Abstract: A method for producing a β-enriched protected decitabine comprising: a) coupling a protected 2-deoxy-ribofuranose with a protected 5-azacytosine in the presence of a catalyst to form a reaction mixture comprising the protected decitabine of formula (I); and b) quenching the reaction mixture of step a) with a base. The β-enriched protected decitabine so made may be deprotected to produce a decitabine product in a high yield and purity.

    Abstract translation: 一种生产富含β-受保护的地西他滨的方法,包括:a)在催化剂存在下,将受保护的2-脱氧 - 呋喃核糖与受保护的5-氮杂胞嘧啶偶联,以形成包含式(I)的受保护的地西他滨的反应混合物; 和b)用碱淬灭步骤a)的反应混合物。 如此制得的富含β的受保护的地西他滨可以脱保护以高产率和高纯度产生地西他滨产物。

    INHIBITION-BASED HIGH-THROUGHPUT SCREEN STRATEGY FOR CELL CLONES
    42.
    发明公开
    INHIBITION-BASED HIGH-THROUGHPUT SCREEN STRATEGY FOR CELL CLONES 有权
    基于抑制的细胞克隆高通量筛选策略

    公开(公告)号:EP2440676A2

    公开(公告)日:2012-04-18

    申请号:EP10785817.7

    申请日:2010-06-10

    Abstract: A method for screening cells with high level expression of a target protein is disclosed. The method includes introducing into a plurality of host cells a DNA construct that encodes both a target protein and an inhibitor to an endogenous selectable marker in the host cells, screening host cells harboring the DNA construct for the expression of the endogenous selectable marker, and isolating cells with reduced expression of the selectable marker. Also disclosed is a DNA construct configured to express both the target protein and the inhibitor inside the host cell.

    Abstract translation: 公开了一种筛选具有高水平表达靶蛋白的细胞的方法。 该方法包括向宿主细胞中引入编码靶蛋白和抑制剂两者的DNA构建体到内源选择标记,筛选携带DNA构建体以表达内源选择标记的宿主细胞,和分离 具有降低的选择标记表达的细胞。 还公开了配置为在宿主细胞内表达靶蛋白和抑制剂的DNA构建体。

    PROCESS FOR THE PREPARATION OF 7-ALKYL-10-HYDROXY-20(S)-CAMPTOTHECIN
    48.
    发明公开
    PROCESS FOR THE PREPARATION OF 7-ALKYL-10-HYDROXY-20(S)-CAMPTOTHECIN 有权
    VERFAHREN ZUR HERSTELLUNG VON 7-烷基-10-羟基-20(S) - 甘露糖胺

    公开(公告)号:EP1628982A4

    公开(公告)日:2006-11-29

    申请号:EP04751971

    申请日:2004-05-12

    CPC classification number: C07D491/22

    Abstract: The key intermediate in any synthesis of Irinotecan is 7-ethyl-10-hydroxy-20(S) camptothecin. A process for the efficient synthesis of this intermediate is demonstrated proceeding through readily availabe 20(S)-camptothecin. Various other tecan compounds may be made by use of corresponding 7-alkyl-10-hydroxy-20(S)-camptothecin intermediates.

    Abstract translation: 伊立替康合成中的关键中间体是7-乙基-10-羟基-20(S)喜树碱。 通过容易地得到20(S) - 喜树碱进行有效合成该中间体的方法。 各种其他的tecan化合物可以通过使用相应的7-烷基-10-羟基-20(S) - 喜树碱中间体来制备。

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