Study On Synthesis Improvement Of Gatifloxacin

Gatifloxacin is a new antimicrobial of quinolones in treatment of respiratory infections showed a high efficacy and good tolerability.The drug in December 1999 was approved the listing,and now listed in more than 40 countries, such as the EU countries, the United States, South America and Central American countries.Because of its difficulty synthesis, most of the current synthetic route at home and abroad has shortcomings there is a low yield and low content. So, the completion of gatifloxacin synthesis and development of its intermediate synthetic route economically viably is quite necessary,and will have very good social and economic prospects.This article reports based on the synthesis method of the literature, done a lot of work to establish synthesis route for large-scale production.The tetrahedron has been reported for the synthesis method and apply for the synthesis patents, in which the synthesis of gatifloxacin is divided into twelve steps. To ensure product purity and yield basis, the paper optimize the twelve-step reaction the operation. So, we removed the toxic, and the difficult post-processing solvent in the synthetic route , replace the raw materials expensive and difficult to purchase, simplifie the purification methods in product line, optimize the synthetic route, improve the total yield from 16.9% to 18.3%, and through a variety of analytical tools, confirme its chemical structure,which have a certain significance to Industrial synthesis of the products.