• 专利标题:   Preparing osimertinib intermediate, comprises carrying out heat reaction of N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine under action of graphene palladium catalyst.
  • 专利号:   CN107746404-A
  • 发明人:   ZHENG G, CUI Z, GAO L, GU H
  • 专利权人:   UNIV JINAN
  • 国际专利分类:   C07D403/04
  • 专利详细信息:   CN107746404-A 02 Mar 2018 C07D-403/04 201826 Pages: 6 Chinese
  • 申请详细信息:   CN107746404-A CN10848005 19 Sep 2017
  • 优先权号:   CN10848005

▎ 摘  要

NOVELTY - Preparing osimertinib intermediate i.e N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine, comprises carrying out heat reaction of N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine (II) under the action of graphene palladium catalyst in a light-emitting diode light illuminated closed container containing aqueous solution, then carrying out hydrogen reduction reaction, and post processing to obtain final product. USE - The method is useful for preparing (I). ADVANTAGE - The method: produces product having yield of more than 95% and purity of more than 98%; has mild reaction conditions; is simple, more efficient, fast and suitable for large scale industrial production; utilizes catalyst which has wear resistance and high repeated utilization rate. DETAILED DESCRIPTION - Preparing osimertinib intermediate i.e N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine of formula (I), comprises carrying out heat reaction of N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine of formula (II) under the action of graphene palladium catalyst in a light-emitting diode light illuminated closed container containing aqueous solution, then carrying out hydrogen reduction reaction, and post processing to obtain final product.