STEREOSELECTIVE PROCESS FOR PREPARING PURINE DIOXOLANE NUCLEOSIDE DERIVATIVES
    18.
    发明申请
    STEREOSELECTIVE PROCESS FOR PREPARING PURINE DIOXOLANE NUCLEOSIDE DERIVATIVES 审中-公开
    制备嘌呤二氧杂环己烷衍生物的立体选择性方法

    公开(公告)号:US20100210840A1

    公开(公告)日:2010-08-19

    申请号:US12670386

    申请日:2008-07-24

    Inventor: Steven J. Coats

    CPC classification number: C07D473/16

    Abstract: A cost-effective process scale method for preparing purine dioxolane nucleoside derivatives in racemic or optically pure form is disclosed, as are nucleoside derivatives prepared by the method. The method involves reacting a purine or a mono- or polysilylated purine derivative with an activated dioxolane analog to produce the dioxolane nucleoside analog in commercially useful yields. Direct reaction of purine or a mono- or polysilylated purine with dioxolanes takes place with highest reported chemical yields and excellent stereoselectivity when an additive in the form of an alpha cyano carbonyl compound or silylated alpha cyano carbonyl compounds is present in the reaction mixture during the glycosylation reaction.

    Abstract translation: 公开了一种用于制备外消旋或光学纯的形式的嘌呤二氧戊环核苷衍生物的成本有效的工艺规模方法,以及通过该方法制备的核苷衍生物。 该方法包括使嘌呤或单或聚硅酸化嘌呤衍生物与活化的二氧杂环戊烷类似物反应,以商业上有效的收率产生二氧戊环核苷类似物。 在糖基化过程中当反应混合物中存在α氰基羰基化合物或甲硅烷基化α氰基羰基化合物形式的添加剂时,嘌呤或单或多聚化嘌呤与二氧戊环的直接反应发生,报道最高的化学产率和优异的立体选择性 反应。

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