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    Methods of Preparing Substituted Tetracyclines with Transition Metal-Based Chemistries
    39.
    发明申请
    Methods of Preparing Substituted Tetracyclines with Transition Metal-Based Chemistries 审中-公开
    用过渡金属基化学制备取代四环素的方法

    公开(公告)号：US20130029943A1

    公开(公告)日：2013-01-31

    申请号：US13312291

    申请日：2011-12-06

    申请人： Mark L. Nelson ,  Glen Rennie ,  Darrell J. Koza

    发明人： Mark L. Nelson ,  Glen Rennie ,  Darrell J. Koza

    IPC分类号： C07C237/26 ,  A61P31/04 ,  A61K31/65

    CPC分类号： C07D295/185 ,  C07C231/12 ,  C07C237/26 ,  C07C2603/46 ,  C07D295/192

    摘要： The present invention relates to novel chemistries which allow for heretofore unobtainable substituted tetracycline compounds which exhibit significant activity in tetracycline responsive states. The methods disclosed herein utilize reactive tetracycline-based precursor compounds, reactive organic substituent precursors and transition metal catalysts under conditions such that a tetracycline compound substituted with the desired organic substituent is formed. In one embodiment of the invention, a substituted tetracycline compound may be prepared by combining a reactive tetracycline-based precursor compound such as an arene tetracycline diazonium salt, and a reactive organic substituent precursor, e.g., alkenes, substituted alkenes, vinyl monomers, aromatics and heteroaromatics, in the presence of a transition metal catalyst, such as palladium chloride, under conditions such that a tetracycline compound substituted with the organic substituent is formed. Such compounds may optionally act as intermediates for making other compounds, e.g., hydrogenation of unsaturated groups on the substituent.

    摘要翻译： 本发明涉及允许迄今为止在四环素反应状态下表现出显着活性的未获得的取代四环素化合物的新化学物质。 本文公开的方法在形成被所需有机取代基取代的四环素化合物的条件下使用基于活性四环素的前体化合物，反应性有机取代基前体和过渡金属催化剂。 在本发明的一个实施方案中，取代的四环素化合物可以通过将活性四环素类前体化合物如芳族四环素重氮盐和反应性有机取代基前体例如烯烃，取代的烯烃，乙烯基单体，芳族化合物和 在过渡金属催化剂如氯化钯存在下，在形成被有机取代基取代的四环素化合物的条件下，进行杂芳族化合物。 这样的化合物可以任选地用作制备其它化合物的中间体，例如取代基上不饱和基团的氢化。