| abstract |
The present invention discloses an intermediate N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-formamidine] that can be used to prepare AZD9291 (I) Phenyl-2-acrylamide (II) and its preparation method. Its preparation steps include: taking 2-fluoro-4-methoxyaniline as the starting material, and preparing N-[2-[[2-(dimethyl Amino)ethyl]methylamino]-4-methoxy-5-carboxamidine]phenyl-2-acrylamide (II). The present invention also discloses a compound of formula II and (2E)-3-dimethylamino-1-(1-methyl-1H-indol-3-yl)-2-propen-1-one (III ) A method for preparing AZD9291 (I) through a cyclization reaction. The preparation method has easy-to-obtain raw materials, simple process, economy and environmental protection, and is suitable for industrialized production. |