1-环丙基-7-氟-8-甲氧基-4-氧代-1,4-二氢喹啉-3-羧酸乙酯与硼酸、乙酐反应得1-环丙基-7-氟-8-甲氧基-4-氧代-1,4-二氢喹啉-3-羧酸根-O~3,O~4-二乙酸根合硼,与(3S,5S)-(5-甲基哌啶-3-基)氨基甲酸叔丁酯经偶联、碱解和酸解“一锅”反应得奈诺沙星,最后成苹果酸盐制得无氟喹诺酮抗菌药苹果酸奈诺沙星,总收率约65%。 Reaction of 1-cyclopropyl-7-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ethyl ester with boronic acid and acetic anhydride gave 1-cyclopropyl-7 Fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylate-O~3, O~4- diacetate boron and (3S, 5S) Methylpiperidin-3-yl) carbamic acid tert-butyl ester by coupling, alkaline hydrolysis and acidolysis “one pot ” reaction was nifloxacin, and finally into a malate salt obtained fluorine-free quinolone antibacterial drugs Nanofloxacin malate, the total yield of about 65%.