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    Intermediates useful for making tetrabenazine compounds
    2.
    发明授权
    Intermediates useful for making tetrabenazine compounds 失效
    可用于制备丁苯那嗪化合物的中间体

    公开(公告)号：US08008500B2

    公开(公告)日：2011-08-30

    申请号：US11760372

    申请日：2007-06-08

    申请人： Michael James Rishel ,  Kande Kankananamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    发明人： Michael James Rishel ,  Kande Kankananamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    IPC分类号： C07D217/00

    CPC分类号： C07D455/06 ,  C07D217/16 ,  C07D217/18 ,  Y02P20/55

    摘要： A method of preparing a tetrabenazine compound (TBZ compound) having structure I comprising the steps of reacting a nucleophilic alkenyl species with aldehyde compound II and oxidizing the resultant allylic alcohol to provide enone III. The protecting group P1 on the tetrahydroisoquinoline nitrogen is removed and the resultant deprotected intermediate is induced to undergo an amino cyclization reaction to provide a product TBZ compound having structure I. The method may be used to prepare either enantiomeric form of tetrabenazine; (+)-tetrabenazine or (−)-tetrabenazine. Alternatively the method may be adapted to provide a mixture enriched in one tetrabenazine enantiomer, a racemic mixture, or a diastereomeric mixture of tetrabenazine compounds. In addition, the present invention provides novel synthetic intermediate compositions which may be used to prepare either or both enantiomers of tetrabenazine, derivatives of tetrabenazine, and analogs of tetrabenazine.

    摘要翻译： 制备具有结构I的丁苯那嗪化合物（TBZ化合物）的方法包括以下步骤：使亲核烯基物质与醛化合物II反应并氧化得到的烯丙基醇以提供烯酮III。 除去四氢异喹啉氮上的保护基P1，将所得脱保护的中间体诱导进行氨基环化反应，得到具有结构I的产物TBZ化合物。该方法可用于制备对映体形式的丁苯那嗪; （+） - 丁苯那嗪或（ - ） - 丁苯那嗪。 或者，该方法可以适于提供富集一种四苯并嗪对映异构体，外消旋混合物或丁苯那嗪化合物的非对映体混合物的混合物。 此外，本发明提供新的合成中间体组合物，其可用于制备丁苯那嗪，丁苯那敏的衍生物和丁苯那嗪的类似物之一或两者的对映异构体。

    Intermediates for fluorinated tetrabenazine carbinol compounds imaging agents and probes
    3.
    发明授权
    Intermediates for fluorinated tetrabenazine carbinol compounds imaging agents and probes 有权
    氟化四苯并嗪甲醇化合物成像剂和探针的中间体

    公开(公告)号：US07919622B2

    公开(公告)日：2011-04-05

    申请号：US11952340

    申请日：2007-12-07

    申请人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    发明人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    IPC分类号： C07D455/06

    CPC分类号： C07D455/06 ,  A61K51/0455 ,  C07B2200/05

    摘要： The present invention provides novel fluorophilic compounds having structure VII wherein R1 is a C1-C20 aliphatic, a C2-C20 cycloaliphatic, or a C2-C20 aromatic radical comprising at least one functional group susceptible to reaction with nucleophilic fluoride ion or an electrophilic fluorinating agent; R2 is a C1-C10 aliphatic radical; R3 is hydrogen or a C1-C10 aliphatic radical; R4 is hydrogen or a C1-C10 aliphatic radical; and R5 is hydrogen, a C1-C10 aliphatic radical, a C2-C10 cycloaliphatic radical, or a C2-C20 aromatic radical. The fluorophilic compounds are provided in both racemic and enantiomerically enriched forms and are useful as intermediates in the preparation of novel PET imaging agents and probes useful in the discovery and performance assessment of PET imaging agents. The fluorophilic compounds are particularly useful in the preparation of PET imaging agents and probes having a high affinity for VMAT-2, a biomarker implicated in human diabetes and other illnesses such as Parkinson's disease.

    摘要翻译： 本发明提供了具有结构VII的新型氟化合物，其中R 1是C 1 -C 20脂族基，C 2 -C 20脂环族或C 2 -C 20芳族基，其包含至少一个易与亲核氟离子反应的官能团或亲电氟化剂 ; R2是C1-C10脂族基团; R3是氢或C1-C10脂族基; R4是氢或C1-C10脂族基; 并且R 5是氢，C 1 -C 10脂族基，C 2 -C 10脂环族基或C 2 -C 20芳族基。 亲氟化合物以外消旋和对映体富集的形式提供，并且可用作制备用于PET成像剂的发现和性能评估的新型PET成像剂和探针的中间体。 亲氟化合物特别可用于制备对VMAT-2具有高亲和力的PET成像剂和探针，所述VMAT-2是涉及人类糖尿病和其它疾病如帕金森病的生物标志物。

    Fluorinated dihydrotetrabenazine ether imaging agents and probes
    4.
    发明授权
    Fluorinated dihydrotetrabenazine ether imaging agents and probes 有权
    氟化二氢丁苯那腈成像剂和探针

    公开(公告)号：US07897770B2

    公开(公告)日：2011-03-01

    申请号：US11923926

    申请日：2007-10-25

    申请人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    发明人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    IPC分类号： C07D455/06

    CPC分类号： C07D455/06 ,  A61K51/0455

    摘要： The present invention provides novel fluorinated ether compounds having structure I wherein R1 is a C2-C10 fluorinated aliphatic radical; R2 is a C1-C10 aliphatic radical, or a C3-C10 cycloaliphatic radical; R3 is hydrogen or a C1-C10 aliphatic radical; and R4 is hydrogen or a C1-C10 aliphatic radical. The fluorinated ether compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The fluorinated ether compounds are shown to possess high affinity for VMAT-2, a biomarker implicated in human diabetes. The fluorinated ether compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabeled fluorinated ether compounds are useful as probes for the discovery of PET imaging agents.

    摘要翻译： 本发明提供具有结构I的新型氟化醚化合物，其中R 1是C 2 -C 10氟化脂族基; R2是C1-C10脂族基团，或C3-C10脂环族基团; R3是氢或C1-C10脂族基; 并且R 4是氢或C 1 -C 10脂族基。 氟化醚化合物以外消旋和对映异构体富集的形式提供，并且可以包含氟-18和氟19中的任一种或两者。显示氟化醚化合物对于涉及人类糖尿病的生物标志物VMAT-2具有高亲和力。 包含氟-18基团的氟化醚化合物可用作靶向VMAT-2生物标志物的PET显像剂。 非放射性标记的氟化醚化合物可用作发现PET成像剂的探针。

    Intermediates for fluorinated dihydrotetrabenazine ether imaging agents and probes
    5.
    发明授权
    Intermediates for fluorinated dihydrotetrabenazine ether imaging agents and probes 有权
    氟化二氢丁苯那嗪醚显像剂和探针的中间体

    公开(公告)号：US07897769B2

    公开(公告)日：2011-03-01

    申请号：US11923805

    申请日：2007-10-25

    申请人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    发明人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    IPC分类号： C07D455/06

    CPC分类号： C07D455/06

    摘要： The present invention provides novel fluorophilic compounds having structure VI wherein R1 is a C2-C20 aliphatic, a C3-C20 cycloaliphatic, or a C3-C20 aromatic radical comprising at least one functional group susceptible to reaction with nucleophilic fluoride ion or an electrophilic fluorinating agent; R2 is a C1-C10 aliphatic radical, or a C3-C10 cycloaliphatic radical; R3 is hydrogen or a C1-C10 aliphatic radical; and R4 is hydrogen or a C1-C10 aliphatic radical. The fluorophilic compounds are provided in both racemic and enantiomerically enriched forms and are useful as intermediates in the preparation of novel PET imaging agents and probes useful in the discovery and performance assessment of PET imaging agents. The fluorophilic compounds are particularly useful in the preparation of PET imaging agents and probes having a high affinity for VMAT-2, a biomarker implicated in human diabetes and other illnesses such as Parkinson's disease.

    摘要翻译： 本发明提供了具有结构VI的新型氟化合物，其中R 1是C 2 -C 20脂族，C 3 -C 20脂环族或C 3 -C 20芳族基，其包含至少一个易于与亲核氟离子反应的官能团或亲电氟化剂 ; R2是C1-C10脂族基团，或C3-C10脂环族基团; R3是氢或C1-C10脂族基; 并且R 4是氢或C 1 -C 10脂族基。 亲氟化合物以外消旋和对映体富集的形式提供，并且可用作制备用于PET成像剂的发现和性能评估的新型PET成像剂和探针的中间体。 亲氟化合物特别可用于制备对VMAT-2具有高亲和力的PET成像剂和探针，所述VMAT-2是涉及人类糖尿病和其它疾病如帕金森病的生物标志物。

    METHOD FOR MAKING TETRABENAZINE COMPOUNDS
    6.
    发明申请
    METHOD FOR MAKING TETRABENAZINE COMPOUNDS 失效
    制备四羧酸化合物的方法

    公开(公告)号：US20080306267A1

    公开(公告)日：2008-12-11

    申请号：US11760359

    申请日：2007-06-08

    申请人： Michael James Rishel ,  Kande Kankananamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    发明人： Michael James Rishel ,  Kande Kankananamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    IPC分类号： C07D455/06

    CPC分类号： C07D455/06 ,  C07D217/16 ,  C07D217/18 ,  Y02P20/55

    摘要： A method of preparing a tetrabenazine compound (TBZ compound) having structure I comprising the steps of reacting a nucleophilic alkenyl species with aldehyde compound II and oxidizing the resultant allylic alcohol to provide enone III. The protecting group P1 on the tetrahydroisoquinoline nitrogen is removed and the resultant deprotected intermediate is induced to undergo an amino cyclization reaction to provide a product TBZ compound having structure I. The method may be used to prepare either enantiomeric form of tetrabenazine; (+)-tetrabenazine or (−)-tetrabenazine. Alternatively the method may be adapted to provide a mixture enriched in one tetrabenazine enantiomer, a racemic mixture, or a diastereomeric mixture of tetrabenazine compounds. In addition, the present invention provides novel synthetic intermediate compositions which may be used to prepare either or both enantiomers of tetrabenazine, derivatives of tetrabenazine, and analogs of tetrabenazine.

    摘要翻译： 制备具有结构I的丁苯那嗪化合物（TBZ化合物）的方法包括以下步骤：使亲核烯基物质与醛化合物II反应并氧化得到的烯丙基醇以提供烯酮III。 除去四氢异喹啉氮上的保护基P1，将所得脱保护的中间体诱导进行氨基环化反应，得到具有结构I的产物TBZ化合物。该方法可用于制备对映体形式的丁苯那嗪; （+） - 丁苯那嗪或（ - ） - 丁苯那嗪。 或者，该方法可以适于提供富集一种四苯并嗪对映异构体，外消旋混合物或丁苯那嗪化合物的非对映体混合物的混合物。 此外，本发明提供新的合成中间体组合物，其可用于制备丁苯那嗪，丁苯那敏的衍生物和丁苯那嗪的类似物之一或两者的对映异构体。

    Method and catalyst system for producing aromatic carbonates
    8.
    发明授权
    Method and catalyst system for producing aromatic carbonates 失效
    用于生产芳族碳酸酯的方法和催化剂体系

    公开(公告)号：US06465675B1

    公开(公告)日：2002-10-15

    申请号：US09677487

    申请日：2000-10-02

    申请人： Grigorii Lev Soloveichik ,  Kirill Vladimirovich Shalyaev ,  Marsha Mottel Grade ,  Bruce Fletcher Johnson

    发明人： Grigorii Lev Soloveichik ,  Kirill Vladimirovich Shalyaev ,  Marsha Mottel Grade ,  Bruce Fletcher Johnson

    IPC分类号： C07C6996

    CPC分类号： B01J23/8926 ,  C07C68/005 ,  C07C69/96

    摘要： A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes an effective amount of a Group VIII B metal source; an effective amount of a bromide composition; an effective amount of an activating organic solvent; an effective amount of a combination of inorganic co-catalysts comprising a lead source and a copper source; and an effective amount of a base.

    摘要翻译： 用于从芳族羟基化合物经济地生产芳族碳酸酯的方法和催化剂体系。 在一个实施方案中，本发明提供了一种通过在包含有效量的VIIIB族金属源的羰基化催化剂体系的存在下使至少一种芳族羟基化合物与氧和一氧化碳接触来羰基化芳族羟基化合物的方法; 有效量的溴化物组成; 有效量的活化有机溶剂; 有效量的包含铅源和铜源的无机助催化剂的组合; 和有效量的碱。