Process for the preparation of substituted aryl pyrazoles
    1.
    发明申请
    Process for the preparation of substituted aryl pyrazoles 审中-公开
    制备取代的芳基吡唑的方法

    公开(公告)号:US20050096354A1

    公开(公告)日:2005-05-05

    申请号:US10932390

    申请日:2004-09-02

    摘要: The present invention relates to a process for the preparation of pesticidal compounds, and more particularly to the preparation of pyrazole compounds. In particular, the present invention relates to a process for preparing 1-arylpyrazoles and 1-pyridylpyrazoles which have pesticidal activity. More particularly, the present invention relates to a novel process by which 3,4,5-trisubstituted 1-arylpyrazoles may be produced directly in a reaction which involves coupling of an aryldiazonium species with an appropriately substituted precursor bearing a desired substituent.

    摘要翻译: 本发明涉及一种制备杀虫化合物的方法,更具体地涉及制备吡唑化合物。 特别地,本发明涉及具有杀虫活性的1-芳基吡唑和1-吡啶基吡唑的制备方法。 更具体地说,本发明涉及一种新的方法,其中3,4,5-三取代的1-芳基吡唑可以直接在涉及使芳基重氮物质与具有所需取代基的适当取代的前体偶联的反应中产生。

    Preparation of triazoles by organometallic addition to ketones and intermediates therefor

    公开(公告)号:US20050272747A1

    公开(公告)日:2005-12-08

    申请号:US11120739

    申请日:2005-05-02

    IPC分类号: A61K31/506 C07D43/02

    CPC分类号: C07D403/06

    摘要: The invention provides a process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reaction of a compound of the formula: wherein R is as previously defined for a compound of the formula (I), with a compound of the formula: wherein R1 and “Het” are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, in the presence of zinc, iodine and/or a Lewis acid and an aprotic organic solvent: said process being optionally followed by conversion of the compound of the formula (I) to an acid addition or base salt thereof.