Patent ID: 10167275

Abstract:
Disclosed are an intermediate, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-formamidine]phenyl-2-propenamide (II), applicable in preparing AZD9291 (I) and a preparation method for the intermediate. Preparation steps of the preparation method comprise: 2-fluoro-4-methoxyaniline, serving as a starting material, undergoes amidation, substitution, nitrification, reduction and guanidination reactions to prepare N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-formamidine]phenyl-2-propenamide (II). Also disclosed is a method for preparing AZD9291 (I) by means of a cyclization reaction between the compound of a formula II and (2E)-3-dimethylamino-1-(1-methyl-1H-indol-3-yl)-2-propen-1-one (III). The preparation method has readily available raw materials and a simple process and is economical, environmentally friendly, and suitable for industrialized production.