2 results about "Bilastine" patented technology

The application discloses a preparation process of bilastine, and belongs to the technical field of medicinal chemistry. The target compound is prepared through three-step chemical reactions by using a folding process, intermediate products do not need to be purified or only need to be simply extracted to remove impurities to meet production requirements; compound I is condensed with compound II in water to prepare compound III; then, a proton acid is added to deprotect to prepare a compound IV aqueous solution; after dichloromethane back extraction to remove impurities; the compound IV aqueous solution is subjected to a substitution reaction with compound V to prepare compound VI. The raw material adopted by the application is clear, cheap and easy to obtain, market supply is stable, the preparation process is simple, water is used as a solvent in the three-step reaction, and no special equipment is required, the production efficiency is improved, the production cycle is shortened, and the generation of three wastes is reduced, and the application is suitable for industrial production; the purity of each intermediate prepared is more than 99%, the purity of the final product can reach 99.88%, and the impurity spectrum is stable and clear.

This application discloses a method for preparing bilastin and its impurities. The method for preparing bilastin includes a reaction step using a compound of formula (I) and / or a salt of a compound of formula (I) as an intermediate, wherein the content of the compound of formula (II) in the intermediate product is not higher than 0.1 wt%. The method of this application yields bilastin with a purity higher than 99.5%, and the content of a single impurity is not more than 0.1%. The purity of the bilastin product meets the quality standards specified in the pharmacopoeia, with a high product qualification rate, which is conducive to large-scale production.