| In this paper, the structure-activity relationship, evolution gradation, the future of research and development were summarized.Pazufloxacin Mesylate, has came into the market in Japan in 2002 firstly, which has a wide clinical usage, the higher blood concentration by intravenously, higher effective speed, lower toxicity of central nervous system. The benefit of the pazufloxatin mesylas is also better than the levofloxacin, norfloxacin, ciprofloxacin, and ofloxacin for the vivo activity of the staphylococcus aureus, especially for the drug resistance. It will be the main product after several products developed. The paper also described the biological activities of Pazufloxcain Mesylate.According to the reports, Pazufloxacin mesylate was synthesized form (s)-9, 10-difluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido-[1,2,3-de] [1,4] benzoxazine-6-carboxylic acid by nucleophilic substitution, cyclic addition, hydrolysis, Hofmann degradation and salt formation with the methane sulfonic acid. The technics has higher rate, simple operating steps, and the shorter period of production, which indicates this synthesis is suitable for the industrial manufacture.
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