Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
    4.
    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:US06545162B1

    公开(公告)日:2003-04-08

    申请号:US09359921

    申请日:1999-07-22

    IPC分类号: C07D20730

    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。

    Method for preparing nitrogen containing compounds
    5.
    发明授权
    Method for preparing nitrogen containing compounds 失效
    含氮化合物的制备方法

    公开(公告)号:US06803472B2

    公开(公告)日:2004-10-12

    申请号:US10296925

    申请日:2002-11-29

    IPC分类号: C07D20730

    摘要: A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitrites or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.

    摘要翻译: 一种合成方法,其包括在甲硅烷基化剂存在下使含NH基的化合物与硫氰酸酯,氰胺,亚硝酸酯或酯反应以合成相应的含氮加成或取代产物。 该方法不仅可以直接有效地合成含氮化合物,包括异硫脲,胍,脒和酰胺,而且还具有广泛的应用范围,适用于大规模合成。

    N-protected synthesis method for use in making porphyrins
    7.
    发明授权
    N-protected synthesis method for use in making porphyrins 失效
    用于制备卟啉的N-保护的合成方法

    公开(公告)号:US06528659B1

    公开(公告)日:2003-03-04

    申请号:US09524621

    申请日:2000-03-13

    IPC分类号: C07D20730

    摘要: One aspect of the present invention relates to a method of forming chemical compounds and, in particular, chemical intermediates having one or more pyrrole sub-units and at least one protecting group bonded to an atom within a pyrrole sub-unit. The method further involves removal of the protecting group so as to provide a desired chemical compound having one or more pyrrole sub-units. The method can be employed in making porphyrin compounds.

    摘要翻译: 本发明的一个方面涉及形成化合物的方法,特别是具有一个或多个吡咯亚单元和至少一个与吡咯亚单元中的原子键合的保护基的化学中间体。 该方法还包括除去保护基,以提供具有一个或多个吡咯亚单元的所需化合物。 该方法可用于制备卟啉化合物。