PROCESS FOR PREPARING AZACYTIDINE INTERMEDIATE
    56.
    发明公开
    PROCESS FOR PREPARING AZACYTIDINE INTERMEDIATE 有权
    制备阿扎地米中间体的方法

    公开(公告)号:EP2324042A1

    公开(公告)日:2011-05-25

    申请号:EP09791228.1

    申请日:2009-08-06

    申请人: Sicor, Inc.

    IPC分类号: C07H19/12 C07H1/00 A61K31/706

    摘要: The present invention provides a processes for preparing 5 -Azacytidine, and intermediates thereof, said process Comprising reacting a silylated 5-azacytosine of the formula (II), a sugar moiety having of the formula (III): and a protic acid; wherein R is a substituted or non substituted C
    1 -C
    20 acyl moiety, R
    1 , R
    2 and R
    3 are each independently H or an alkyl group, and X is a halogen. The present invention further provides an analytical method for determining the purity of 5-Azacytidine in a sample.

    摘要翻译: 本发明提供了用于制备5-氮杂胞苷及其中间体的方法,所述方法包括使式(II)的甲硅烷基化5-氮杂胞嘧啶,具有式(III)的糖部分和质子酸反应; 其中R为取代或未取代的C 1 -C 20酰基部分,R 1,R 2和R 3各自独立地为H或烷基,并且X为卤素。 本发明进一步提供了确定样品中5-氮杂胞苷纯度的分析方法。