The invention belongs to the technical field of
organic synthesis, and provides an oxiratinib intermediate and a preparation method thereof, and a preparation method of oxiratinib. The preparation method comprises the following steps: taking p-chlorobenzyl
chloride as a
raw material, reacting with
sodium sulfite to obtain the
sodium 4-chlorobenzenemethanesulfonate, then taking the
sodium 4-chlorobenzenemethanesulfonate as a
raw material, and carrying out reactions such as first
methylamine substitution, hydrogenation reduction, condensation, chlorination,
dimethylamine substitution and the like to obtain the sodium 4-chlorobenzenemethanesulfonate. The p-chlorobenzyl
chloride is used as a starting
raw material, and compared with p-bromobenzyl
bromide used as a raw material in the prior art, the raw material is easy to obtain, low in cost and more suitable for industrial production. And meanwhile, after the chlorination reaction, the obtained chlorination reaction feed liquid is directly added into the
dimethylamine aqueous solution to carry out the
dimethylamine reaction without post-treatment, so that the post-treatment is simple, and time and labor are saved. Besides, the
cuprous salt is combined with the ligand to catalyze the
substitution reaction of the first
methylamine, so that the yield of the 4-methylaminobenzene
methanesulfonic acid is increased, and finally, the yield of the olotinib is increased.