NOVEL MANUFACTURING PROCESS FOR TRIAZINE, PYRIMIDINE AND PYRIDINE DERIVATIVES
    61.
    发明申请
    NOVEL MANUFACTURING PROCESS FOR TRIAZINE, PYRIMIDINE AND PYRIDINE DERIVATIVES 审中-公开
    吡啶,吡嗪和吡啶衍生物的新型制备方法

    公开(公告)号:WO2015162084A1

    公开(公告)日:2015-10-29

    申请号:PCT/EP2015/058493

    申请日:2015-04-20

    摘要: The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I), wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5- triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

    摘要翻译: 本发明涉及一种制备式(I)的三嗪,嘧啶和吡啶衍生物的方法,其中U,V,W和Z是氮或碳原子,其中U,V和W中的至少一个是氮,而另一个 取代基如本说明书所定义,通过将一种类型的Suzuki偶联中的相应的卤代 - 三嗪,嘧啶或吡啶与吡啶基或嘧啶基 - 硼烷缩合,其中氨基官能团被保护为甲脒。 本发明进一步涉及合适的中间体及其制备方法。 此外,本发明涉及固体形式的纯的5-(4,6-二吗啉代-1,3,5-三嗪-2-基)-4-(三氟甲基)吡啶-2-胺。