Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
    5.
    发明授权
    Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 有权
    在固体支持物上合成吡咯和咪唑甲酰胺的方法

    公开(公告)号:US06683189B1

    公开(公告)日:2004-01-27

    申请号:US09360344

    申请日:1999-07-22

    IPC分类号: C07D23102

    摘要: The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

    摘要翻译: 本发明描述了一种固相合成含有咪唑和吡咯甲酰胺的聚酰胺的新方法。 聚酰胺在固体载体上由芳族羧酸和芳族胺制备,具有高逐步偶联收率(> 99%),提供毫克量的高纯度聚酰胺。 本发明还描述了天然产物Netropin和Distamycin A的类似物的合成,两种抗病毒抗生素。 本发明还描述了咪唑和吡咯甲酰胺聚酰胺 - 寡核苷酸共轭物的固相合成的新方法。 该方法将大大增加可合成和测试的次槽结合聚酰胺和次槽结合聚酰胺 - 寡核苷酸缀合物的复杂性和数量。