Industrially scalable nucleoside synthesis
    5.
    发明授权
    Industrially scalable nucleoside synthesis 失效
    工业可扩展的核苷合成

    公开(公告)号:US07595390B2

    公开(公告)日:2009-09-29

    申请号:US10833925

    申请日:2004-04-28

    IPC分类号: C07H19/073

    CPC分类号: C07H19/073

    摘要: An industrially scalable two-step process for preparing a β-L-2′-deoxy-nucleoside that results in a predominance of the β- over the α-anomeric form of the compound is described. An optional third step may be used to prepare 3′-prodrugs of desirable β-L-2′-deoxy-nucleosides for the delivery of these pharmaceuticals effective for treating viral diseases. The synthetic process is applicable in particular to the formation of β-L-2′-deoxy-cytidine, a pharmaceutically acceptable salt or prodrug thereof. The process can provide a relatively uncontaminated product that may require no further isolation or purification, thereby making the synthesis easily scalable for industrial manufacture.

    摘要翻译: 描述了一种用于制备β-L-2'-脱氧核苷的工业可扩展的两步法,其导致β-位于化合物的α-端基异构体形式的优势。 可选的第三步可用于制备所需的β-L-2'-脱氧核苷的3'-前药,用于递送有效治疗病毒性疾病的这些药物。 合成方法特别适用于形成β-L-2'-脱氧胞苷,其药学上可接受的盐或前药。 该方法可以提供可能不需要进一步分离或纯化的相对未污染的产品,从而使合成容易扩展到工业制造。