盐酸加替沙星的合成研究  

Synthesis research of gatifloxacin hydrochloride.

作　　者：顾海宁[1] 蒋永祥 汪劲松[3] 

机构地区：[1]浙江大学分析测试中心,浙江杭州310028 [2]湖州出入境检验检疫局,浙江湖州313000 [3]杭州广林生物医药有限公司,浙江杭州310028

出　　处：《浙江大学学报（理学版）》2005年第1期66-68,74,共4页Journal of Zhejiang University（Science Edition）

摘　　要：以2,4,5-三氟-3-甲氧基苯甲酸为起始原料,经酰氯化后与N,N-二甲氨基丙烯酸乙酯偶联,环丙胺置换、环合水解、与2-甲基哌嗪缩合、水解成盐制得本品,总收率为41.1%.本合成工艺原料易得,操作简单,是一种新的合成加替沙星的方法.Gatifloxacin was prepared from 3-methoxy-2,4,5-triflurobenzoic acid by acylating reaction, followed by coupling with Ethyl N,N-dimethylaminoacrylate, displacement with cyclopropyl amine, cyclization, hydrolysis, condensation with 2-methylpiperazine, hydrolysis, and salification, successively. The total yield was 41.1%. The materials were easily obtained and the operation was easily controlled.

关 键 词：加替沙星 中间体 氟喹诺酮 合成 

分 类 号：O621.3[理学—有机化学] TQ463.25[理学—化学]