首页> 外国专利> Method of preparing a substituted tetracycline compound, reactive chemical tetracycline complex, 7-substituted tetracycline compound, and, 9-substituted tetracycline compound

Method of preparing a substituted tetracycline compound, reactive chemical tetracycline complex, 7-substituted tetracycline compound, and, 9-substituted tetracycline compound

机译:制备取代四环素化合物,反应性化学四环素配合物,7-取代四环素化合物和9-取代四环素化合物的方法

摘要

"METHOD OF PREPARING A REPLACED TETRACYCLINE COMPOUND, TETRACYCLINE REACTIVE CHEMICAL COMPLEX 7-REPLACED TETRACYCLINE COMPOUND, AND 9-REPLACED TETRACYCLINE COMPOUND". The present invention relates to new chemistries that have so far not allowed to obtain substituted tetracycline compounds, which exhibit significant antibacterial activity. The methods described here use reactive tetracycline-based precursor compounds, reactive organic substituent precursors and transition metal catalysts, under conditions such that a tetracycline compound, substituted by the desired organic substituent, is formed. In one version of the invention, a substituted tetracycline compound can be prepared by combining a reactive tetracycline-based precursor compound, such as a tetracycline arene diazonium salt and a reactive organic substituent precursor, e.g. 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 by the organic substituent, is formed. Such compounds can optionally act as intermediates to produce other compounds, e.g. hydrogenation of unsaturated groups of the substituent.
机译:“制备取代的四环素化合物,四环素反应性化学络合物7取代的四环素化合物和9取代的四环素化合物的方法”。本发明涉及迄今为止尚未获得具有显着抗菌活性的取代四环素化合物的新化学方法。在此描述的方法使用反应性的基于四环素的前体化合物,反应性的有机取代基前体和过渡金属催化剂,条件是形成被所需的有机取代基取代的四环素化合物。在本发明的一种形式中,可以通过将基于反应性四环素的前体化合物(例如四环素芳烃重氮盐)和反应性有机取代基前体例如碳酸氢钠组合来制备取代的四环素化合物。在过渡金属催化剂如氯化钯的存在下,在形成被有机取代基取代的四环素化合物的条件下,例如烯烃,取代的烯烃,乙烯基单体,芳族化合物和杂芳族化合物。这样的化合物可以任选地用作产生其他化合物的中间体,例如取代基的不饱和基团的氢化。

著录项

  • 公开/公告号BR0013993A

    专利类型

  • 公开/公告日2002-07-02

    原文格式PDF

  • 申请/专利权人 TRUSTEES OF TUFTS COLLEGE;

    申请/专利号BR20000013993

  • 申请日2000-09-13

  • 分类号C07C237/26;C07C231/12;A61K31/65;A61P31/04;

  • 国家 BR

  • 入库时间 2022-08-22 00:46:11

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