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    Methods to manufacture 1,3-dioxolane nucleosides
    5.
    发明授权
    Methods to manufacture 1,3-dioxolane nucleosides 有权
    1,3-二氧戊环核苷的制备方法

    公开(公告)号：US08420354B2

    公开(公告)日：2013-04-16

    申请号：US12870319

    申请日：2010-08-27

    申请人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Cleary ,  Amir Pesyan

    发明人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Cleary ,  Amir Pesyan

    IPC分类号： C12P19/00 ,  C12P19/38 ,  C12P19/40 ,  C07D239/00 ,  C07D239/02 ,  C07D473/00

    CPC分类号： C07D473/16 ,  C07D317/34 ,  C07D405/04

    摘要： This application provides a process for preparing enantiomerically pure β-D-dioxolane nucleosides. In particular, a new synthesis of (−)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure β-D- or β-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected β-D- or β-L-1,3-dioxolane nucleoside.

    摘要翻译： 本申请提供了制备对映异构体纯的对二氧戊环核苷的方法。 特别地，描述了适用于大规模开发的（ - ） - DAPD的新合成。 在一个实施方案中，本发明提供了制备基本上纯的二 - 或 - bgr--L-1,3-二氧戊环核苷的方法，其包括a）制备或获得酯化的2,2-二烷氧基乙醇; b）用乙醇酸环化酯化的2,2-二烷氧基乙醇得到1,3-二氧戊环内酯; c）拆分1,3-二氧戊环内酯以获得基本上纯的D-或L-内酯; d）选择性还原和活化D-或L-手性内酯，得到基本上纯的D-或L-1,3-二氧戊环; e）将D-或L-1,3-二氧戊环与活化和/或受保护的嘌呤或嘧啶碱基偶联; 和f）任选地纯化所述核苷以获得基本上纯的保护的-β-或 - bgr; -L-1,3-二氧戊环核苷。

    Methods to Manufacture 1,3-Dioxolane Nucleosides
    6.
    发明申请
    Methods to Manufacture 1,3-Dioxolane Nucleosides 有权
    1,3-二氧戊环核苷的制备方法

    公开(公告)号：US20110130559A1

    公开(公告)日：2011-06-02

    申请号：US12870319

    申请日：2010-08-27

    申请人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Cleary ,  Amir Pesyan

    发明人： Marcos Sznaidman ,  George R. Painter ,  Merrick R. Almond ,  Darryl G. Cleary ,  Amir Pesyan

    IPC分类号： C07H19/16

    CPC分类号： C07D473/16 ,  C07D317/34 ,  C07D405/04

    摘要： This application provides a process for preparing enantiomerically pure β-D-dioxolane nucleosides. In particular, a new synthesis of (−)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure β-D- or β-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected β-D- or β-L-1,3-dioxolane nucleoside.

    摘要翻译： 本申请提供了制备对映异构体纯的对二氧戊环核苷的方法。 特别地，描述了适用于大规模开发的（ - ） - DAPD的新合成。 在一个实施方案中，本发明提供了制备基本上纯的二 - 或 - bgr--L-1,3-二氧戊环核苷的方法，其包括a）制备或获得酯化的2,2-二烷氧基乙醇; b）用乙醇酸环化酯化的2,2-二烷氧基乙醇得到1,3-二氧戊环内酯; c）拆分1,3-二氧戊环内酯以获得基本上纯的D-或L-内酯; d）选择性还原和活化D-或L-手性内酯，得到基本上纯的D-或L-1,3-二氧戊环; e）将D-或L-1,3-二氧戊环与活化和/或受保护的嘌呤或嘧啶碱基偶联; 和f）任选地纯化所述核苷以获得基本上纯的保护的β-和/或b-l-1,3-二氧戊环核苷。