A SINGLE STEP ENANTIOSELECTIVE PROCESS FOR THE PREPARATION OF 3-SUBSTITUTED CHIRAL PHTHALIDES
    1.
    发明申请
    A SINGLE STEP ENANTIOSELECTIVE PROCESS FOR THE PREPARATION OF 3-SUBSTITUTED CHIRAL PHTHALIDES 审中-公开
    制备3-取代的手性邻苯二甲酸酯的一步非对称选择性方法

    公开(公告)号:WO2013072830A1

    公开(公告)日:2013-05-23

    申请号:PCT/IB2012056340

    申请日:2012-11-12

    CPC classification number: C07D307/88 C07B53/00 C07D307/92 C07D493/04

    Abstract: The present invention discloses single step, highly enantioselective catalytic oxidative cyclization process for the synthesis of 3-substituted chiral phthalides. In particular, the invention discloses asymmetric synthesis of chiral phthalides via synergetic nitrile accelerated oxidative cyclization of o-cyano substituted aryl alkenes in high yield and enantiomeric excess (ee) in short reaction time. Also, disclosed herein is "one -pot" asymmetric synthesis of biologically important natural compounds having 3-substituted chiral phthalide structural framework in the molecule.

    Abstract translation: 本发明公开了用于合成3-取代的手性苯酞的单步高度对映选择性催化氧化环化方法。 特别地,本发明公开了通过在短反应时间内以高收率和对映体过量(ee)协同腈促进氧化环化邻氰基取代的芳基烯烃来手性苯酞的不对称合成。 此外,本文公开的是分子中具有3-取代的手性苯酞结构骨架的生物学上重要的天然化合物的“一锅法”不对称合成。

    A SINGLE STEP ENANTIOSELECTIVE PROCESS FOR THE PREPARATION OF 3-SUBSTITUTED CHIRAL PHTHALIDES
    2.
    发明申请
    A SINGLE STEP ENANTIOSELECTIVE PROCESS FOR THE PREPARATION OF 3-SUBSTITUTED CHIRAL PHTHALIDES 审中-公开
    用于制备3-取代的手性对苯二甲酸酯的单步选择性方法

    公开(公告)号:WO2013072830A4

    公开(公告)日:2013-08-22

    申请号:PCT/IB2012056340

    申请日:2012-11-12

    CPC classification number: C07D307/88 C07B53/00 C07D307/92 C07D493/04

    Abstract: The present invention discloses single step, highly enantioselective catalytic oxidative cyclization process for the synthesis of 3-substituted chiral phthalides. In particular, the invention discloses asymmetric synthesis of chiral phthalides via synergetic nitrile accelerated oxidative cyclization of o-cyano substituted aryl alkenes in high yield and enantiomeric excess (ee) in short reaction time. Also, disclosed herein is "one -pot" asymmetric synthesis of biologically important natural compounds having 3-substituted chiral phthalide structural framework in the molecule.

    Abstract translation: 本发明公开了用于合成3-取代的手性苯并二氮杂环酮的单步高度对映选择性催化氧化环化方法。 特别地,本发明公开了通过协同腈在低反应时间内以高收率和对映异构体过量(ee)加速氧化环化邻氰基取代的芳族烯烃的不对称合成方法。 此外,本文公开了在分子中具有3-取代的手性苯并二氮苯结构框架的生物重要天然化合物的“一 - ”不对称合成。

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