公开(公告)号：US20130338358A1

公开(公告)日：2013-12-19

申请号：US13981118

申请日：2012-01-27

申请人： Kazuyoshi Obitsu ,  Takahiro Akiba ,  Koji Kobayashi ,  Shun Hirasawa ,  Yutaka Kondoh ,  Kazuhiro Takeguchi ,  Vuji Takahama ,  Ryoki Orii

发明人： Kazuyoshi Obitsu ,  Takahiro Akiba ,  Koji Kobayashi ,  Shun Hirasawa ,  Yutaka Kondoh ,  Kazuhiro Takeguchi ,  Vuji Takahama ,  Ryoki Orii

IPC分类号： C07D401/12 ,  C07D211/44

CPC分类号： C07D401/12 ,  C07D211/44

摘要： Provided is a method for producing a di(arylamino)aryl compound that has superior inhibitory activity against the kinase activities of EML4-ALK fusion protein and mutant EGFR protein and is useful as an active ingredient in pharmaceutical compositions for cancer treatment. The production method includes no purification step using silica gel column chromatography or no step possibly producing a mutagenic mesylate ester as a by-product, greatly improves overall yield, and is high yield and low cost and suitable for the industrial production of pharmaceutical products. Also provided is a synthetic intermediate that is useful in the production method.

摘要翻译： 提供了对于EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有优异抑制活性的二（芳基氨基）芳基化合物的制造方法，可用作癌症治疗用药物组合物中的有效成分。 制造方法不包括使用硅胶柱色谱法的纯化步骤，或者没有可能产生作为副产物的诱变甲磺酸酯的步骤，大大提高了总产率，并且产率高，成本低，适合于药品的工业化生产。 还提供了在生产方法中有用的合成中间体。