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    ASYMMETRIC SYNTHESIS OF ROCAGLAMIDES VIA ENANTIOSELECTIVE PHOTOCYCLOADDITION MEDIATED BY CHIRAL BRONSTED ACIDS
    3.
    发明申请
    ASYMMETRIC SYNTHESIS OF ROCAGLAMIDES VIA ENANTIOSELECTIVE PHOTOCYCLOADDITION MEDIATED BY CHIRAL BRONSTED ACIDS 有权
    不对称合成通过由CHIRAL BRONSTED ACIDS介导的选择性光合作用的聚酰胺

    公开(公告)号：US20120238766A1

    公开(公告)日：2012-09-20

    申请号：US13423370

    申请日：2012-03-19

    申请人： John A. Porco, JR. ,  Baudouin Gerard

    发明人： John A. Porco, JR. ,  Baudouin Gerard

    IPC分类号： C07D307/93 ,  C07D311/94 ,  C07D313/08

    CPC分类号： C07D317/12 ,  C07D307/93 ,  C07D317/72 ,  C07D493/08 ,  C07D493/10

    摘要： The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

    摘要翻译： 本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。 合成方法通常涉及在3-羟基色酮衍生物中光化学生成氧化吡啶鎓物质，随后在TADDOL衍生物存在下，将氧化吡啶类物质的对映选择性1,3-偶极环加成到偶极嗜酸细胞。 该方法可用于形成含有阿格林核心结构的加合物。 还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。 本发明还涉及用于制造用于治疗癌症或癌症病症的药物，与细胞过度增殖相关的疾病或NF-和B受体依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

    SYNTHESIS OF ROCAGLAMIDE NATURAL PRODUCTS VIA PHOTOCHEMICAL GENERATION OF OXIDOPYRYLIUM SPECIES
    7.
    发明申请
    SYNTHESIS OF ROCAGLAMIDE NATURAL PRODUCTS VIA PHOTOCHEMICAL GENERATION OF OXIDOPYRYLIUM SPECIES 审中-公开
    通过氧化亚光谱物种的光化学生成合成山梨酰胺天然产物

    公开(公告)号：US20110065786A1

    公开(公告)日：2011-03-17

    申请号：US12900874

    申请日：2010-10-08

    申请人： John A. Porco, JR. ,  Baudouin Gerard ,  Guilford Jones, II

    发明人： John A. Porco, JR. ,  Baudouin Gerard ,  Guilford Jones, II

    IPC分类号： A61K31/343 ,  C07D307/77 ,  A61P35/00

    CPC分类号： C07D307/93 ,  C07D311/30 ,  C07D313/08 ,  C07D493/08

    摘要： The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

    摘要翻译： 本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。 特别地，新的仿生合成方法包括从3-羟基色酮衍生物光化学生成氧化吡啶鎓物质，随后将氧化吡啶类物质偶氮环加成到偶极子体。 该方法可用于形成含有阿格林核心结构的加合物。 还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。 本发明还涉及用于制造用于治疗癌症或癌性病症的药物，与细胞过度增殖相关的病症或NF-和B受体依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

    Asymmetric Synthesis of Rocaglamides via Enantioselective Photocycloaddition Mediated by Chiral Bronsted Acids
    9.
    发明申请
    Asymmetric Synthesis of Rocaglamides via Enantioselective Photocycloaddition Mediated by Chiral Bronsted Acids 有权
    通过手性布朗斯台德酸介导的对映选择性光环加成反应的罗卡胶的非对称合成

    公开(公告)号：US20090299081A1

    公开(公告)日：2009-12-03

    申请号：US12301727

    申请日：2007-05-21

    申请人： John A. Porco, JR. ,  Baudouin Gerard

    发明人： John A. Porco, JR. ,  Baudouin Gerard

    IPC分类号： C07D307/77 ,  C07D313/06

    CPC分类号： C07D317/12 ,  C07D307/93 ,  C07D317/72 ,  C07D493/08 ,  C07D493/10

    摘要： The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

    摘要翻译： 本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。 合成方法通常涉及在3-羟基色酮衍生物中光化学生成氧化吡啶鎓物质，随后在TADDOL衍生物存在下，将氧化吡啶类物质的对映选择性1,3-偶极环加成到偶极嗜酸细胞。 该方法可用于形成含有阿格林核心结构的加合物。 还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。 本发明还涉及用于制造用于治疗癌症或癌症病症的药物，与细胞过度增殖相关的疾病或NF-κB依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。