The invention belongs to the technical field of
chemical synthesis, and particularly relates to a
rupatadine fumarate intermediate and a preparation method of
rupatadine fumarate. The method comprises the following steps: (1) reacting a compound shown in a formula VI with a halogenating
reagent to obtain a
rupatadine fumarate intermediate shown in a formula V; (2) adding the intermediate of formula V and a compound of formula IV into an acid-binding agent for reaction to obtain a compound of formula III; (3) reacting the compound in the formula III with a
reducing agent to obtain a compound in a formula II; and (4) reacting the compound shown in the formula II with
fumaric acid to obtain rupatadine fumarate. According to the preparation method, 3, 5-dimethylpyridine-N-
oxide is used for carrying out bromination or chlorination, and compared with bromination or chlorination carried out by using 3, 5-dimethylpyridine, the purity and the yield of a halogenated product are higher. Moreover, after the compound shown in the formula V reacts with the compound shown in the formula IV,
column chromatography is not needed, the compound shown in the formula III is obtained through
solvent refining, post-treatment operation is simple, and industrial production is facilitated.