苹果酸奈诺沙星的合成  

Synthesis of Nemonoxacin Malate

作　　者：陈钢[1] 盛力[1] 邹先岩 毛伟[1] 

机构地区：[1]浙江医药股份有限公司新昌制药厂,浙江新昌312500 [2]太景生物科技股份有限公司,中国台湾台北11470

出　　处：《中国医药工业杂志》2014年第2期101-103,共3页Chinese Journal of Pharmaceuticals

摘　　要：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%。Ethyl 1-cyclopropyl_7.fluoro_8-methoxyl-4-oxo-l,4-dihydroquinoline-3-carboxylate was reacted with boric acid and acetic anhydride to give 1-cyclopropyl-7.fluoro-8-methoxy-4-oxo-l,4-dihydroquinoline-3-carboxylic- O3,O4-diacetyl boron complex, which was coupled with tert-butyl （3S,5S） - （5-methylpeperidin-3-yl） carbamate and then hydrolyzed by sodium hydroxide and hydrochloric acid separately to provide nemonoxacin in one pot. Nemonoxacin malate, a nonflourinated quinolone antibacterial agent, was obtained by salt formation with an overall yield of about 65 %.

关 键 词：奈诺沙星 无氟喹诺酮 抗菌药 合成 

分 类 号：R978.1[医药卫生—药品]