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 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2014年第2期101-103,共3页
Chinese Journal of Pharmaceuticals
关键词
奈诺沙星
无氟喹诺酮
抗菌药
合成
nemonoxacin
nonflourinated quinolone
antibacterial agent
synthesis
