▎ 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.