普卢利沙星的合成  

Synthesis of prulifloxacin

作　　者：马淑涛[1] 张建礼 王二兵[1] 王其蕊[1] 

机构地区：[1]山东大学药学院,山东济南250012 [2]山东齐都药业有限公司,山东淄博255400

出　　处：《中国药物化学杂志》2005年第6期347-350,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的改进氟喹诺酮类抗菌药普卢利沙星的合成工艺。方法以3,4-二氟苯胺为起始原料经过8步反应制得关键中间体(±)6,7-二氟-1-甲基-4-氧代-1H,4H-[1,3]硫氮杂环丁烷并[3,2-a]喹啉-3-羧酸乙酯(10),化合物10经氢氧化钾水解,然后与4-(1-哌嗪基)甲基-5-甲基-2-氧代-1,3-二氧杂环戊烯(15)反应合成普卢利沙星。结果与结论合成的普卢利沙星的结构经元素分析和1H-NMR确证,总收率为18.6%。Aim To improve the synthetic procedure of prulifloxacin. Methed The key intermediate （ ＋ ）ethyl 6, 7-difluoro-l-methyl-4-oxo-1 H, 4H-[ 1,3 ]thiazeto[ 1,3-a]quinoline-3-carboxylate（10）was obtained by using 3, 4-dlfluoroaniline as starting material in 8 steps. After hydrolysis in the presence of potassium hydroxide, the intermediate 10 can be reacted with 4-（1-piperazine）methyl-5-methylene-1, 3-dioxolane- 2-one （15）to give prulifloxacin. Results and conclusions The target compound was synthesized and its structure was identified by elemental analysis and ^1H-NMR, and the overall yield was 18.6%.

关 键 词：药物化学 药物制备 化学合成 普卢利沙星 氟喹诺酮 抗菌药 

分 类 号：R914.5[医药卫生—药物化学] R978.1[医药卫生—药学]