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| 盐酸加替沙星的合成研究 | |
| 引用本文： | 顾海宁,蒋永祥,汪劲松.盐酸加替沙星的合成研究[J].浙江大学学报(理学版),2005,32(1):66-68,74. |
| 作者姓名： | 顾海宁 蒋永祥 汪劲松 |
| 作者单位： | 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 |
| 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. |
| 关 键 词： | 加替沙星 中间体 氟喹诺酮 合成 |
| 文章编号： | 1008-9497(2005)01-066-03 |
Synthesis research of gatifloxacin hydrochloride |
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| GU Hai-ning,JIANG Yong-xiang,WANG Jin-song.Synthesis research of gatifloxacin hydrochloride[J].Journal of Zhejiang University(Sciences Edition),2005,32(1):66-68,74. | |
| Authors: | GU Hai-ning JIANG Yong-xiang WANG Jin-song |
| Institution: | GU Hai-ning~1,JIANG Yong-xiang~2,WANG Jin-song~3 |
| Abstract: | 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. |
| Keywords: | gatifloxacin Intermediate fluoroquinolone synthesis |
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