- Novel preparation method of epidermal growth factor receptor (EGFR) inhibitor neratinib
-
The invention relates to a preparation method of an epidermal growth factor receptor (EGFR) inhibitor neratinib. The method is characterized in that 6-[(E)-4-(dimethylamino)-2-butenylamido]-7-ethoxy-4-chloro-3-quinolylmethylnitrile (I) continuously reacts with 2-chloro-3-aminophenol (II) and dichloromethylpyridine hydrochloride (III) to temporarily obtain an intermediate (E)-N-{4-[3-chloro-4-hydroxyanilino]3-cyno-5-ethoxy-6-quinolyl}-4-dimethylamino-2-butenylamide (IV) in order to finally obtain neratinib. The preparation method adopts a continuous reaction process, and dichloromethylpyridine hydrochloride (III) is a catalyst in the first stage of the continuous reaction and is a reaction reagent in the second stage of the continuous reaction, so the method has the advantages of simple and easily available raw materials, high yield, mild reaction conditions, extremely small amount of a generated waste liquid, and high facilitation of industrial production of the above raw medicine.
- -
-
Paragraph 0030; 0031
(2016/11/21)
-