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12 条记录 (耗时 0.024 秒)

    Traceless solid phase synthesis of indole derivatives
    3.
    发明授权
    Traceless solid phase synthesis of indole derivatives 失效
    无痕固相合成吲哚衍生物

    公开(公告)号：US5919947A

    公开(公告)日：1999-07-06

    申请号：US145692

    申请日：1998-09-02

    申请人： Adrian Leonard Smith

    发明人： Adrian Leonard Smith

    IPC分类号： C07D209/08 ,  C07D209/12 ,  C07D209/14

    CPC分类号： C07D209/08 ,  C07D209/12 ,  C07D209/14

    摘要： The present invention relates to a traceless solid phase process for the preparation of an indole derivative, which comprises the following steps:(1) reaction of an optionally substituted 2-iodoaniline derivative via the nitrogen atom of the NH.sub.2 moiety thereof with a dihydropyran-functionalized polymeric resin under conditions effective to form an aminal linkage;(2) reaction of the tetrahydropyran aminal derivative thereby obtained with an acetylene derivative in the presence of a transition metal catalyst under conditions effective to promote indole formation;(3) treatment of the product thereby obtained with acid, whereby the aminal linkage is cleaved and the desired indole derivative is liberated from the resin; and(4) isolation of the desired indole derivative thereby obtained.

    摘要翻译： 本发明涉及一种用于制备吲哚衍生物的无痕固相法，其包括以下步骤：（1）通过其NH 2部分的氮原子将任选取代的2-碘苯胺衍生物与二氢吡喃官能化的 聚合物树脂在有效形成氨基键的条件下; （2）由此得到的四氢吡喃二胺衍生物与乙炔衍生物在过渡金属催化剂存在下在有效促进吲哚形成的条件下反应; （3）用酸处理由此得到的产物，由此使所述的二胺键断裂并从所述树脂中释出所需的吲哚衍生物; 和（4）所得吲哚衍生物的分离。

    Chemical synthesis of 1,3-disubstituted quinazolinediones
    10.
    发明授权
    Chemical synthesis of 1,3-disubstituted quinazolinediones 失效
    化学合成1,3-二取代喹唑啉二酮

    公开(公告)号：US5783698A

    公开(公告)日：1998-07-21

    申请号：US779498

    申请日：1997-01-07

    申请人： Adrian Leonard Smith

    发明人： Adrian Leonard Smith

    IPC分类号： C07D239/96 ,  C07D239/54

    CPC分类号： C07D239/96

    摘要： The present invention relates to a method for the synthesis of 1,3-disubstituted quinazolinedione derivatives which comprises: (a) reacting a haloformate functionalized polystyrene resin with a substituted anthranilic acid derivative under conditions effective to form a urethane-linkage; (b) reacting the product of step (a) with a primary amine under conditions effective to form an anthranilamide derivative; (c) heating the anthranilamide to effect intramolecular cyclization thereby liberating the 1,3-disubstituted quinazolinedione derivative from the resin into solution; and (d) isolating the 1,3-disubstituted quinazolinedione by filtration and solvent removal.

    摘要翻译： 本发明涉及1,3-二取代喹唑啉二酮衍生物的合成方法，其包括：（a）在有效形成氨基甲酸酯键的条件下，使卤代甲酸酯官能化聚苯乙烯树脂与取代的邻氨基苯甲酸衍生物反应; （b）在有效形成邻氨基苯甲酰胺衍生物的条件下使步骤（a）的产物与伯胺反应; （c）加热邻氨基苯甲酰胺进行分子内环化，从而将1,3-二取代的喹唑啉二酮衍生物从树脂释放到溶液中; 和（d）通过过滤和溶剂去除分离1,3-二取代的喹唑啉二酮。