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加替沙星合成工艺改进研究
引用本文:李倩,赵世明,罗振福,孙有光.加替沙星合成工艺改进研究[J].精细化工中间体,2009,39(5):37-40.
作者姓名:李倩  赵世明  罗振福  孙有光
作者单位:1. 天津理工大学化学与化工工程学院,天津,300384
2. 天津药物研究院化学制药研究部,天津,300193
摘    要:以3,4,5,6-四氟苯二甲酸为起始原料,依次经水解、脱羧、甲基化、酰化、缩合、脱羧、丙胺酯、环合、硼酯化及缩哌反应得到加替沙星。总收率为18.3%(以3,4,5,6-四氟苯二甲酸计),并对合成工艺进行了优化,工艺适合于工业化生产。

关 键 词:3  4  5  6-四氟苯二甲酸  合成  优化

Process Imporvement of Synthesis of Gatifloxacin
LI Qian,ZHAO Shi-ming,LUO Zhen-fu,SUN You-guang.Process Imporvement of Synthesis of Gatifloxacin[J].Fine Chemical Intermediates,2009,39(5):37-40.
Authors:LI Qian  ZHAO Shi-ming  LUO Zhen-fu  SUN You-guang
Affiliation:LI Qian , ZHAO Shi-ming, LUO Zhen-fu, SUN You-guang(1. School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China; 2. Chemical Pharmaceuticals Department, Tianjin Pharmaceutical Research Institute, Tianjin 300193, China)
Abstract:Title compound was prepared starting from 3,4,5,6-tetrafluorophthalic acid via hydrolysis, decarboxylation, methylation, acylation, condensation, decarboxylation, propylamine esters, cyclization, boron esterification and condensation with piperazine in an overal yield of 18.3%. The reaction conditions were optimized, which are adaptable to industrial scale-up.
Keywords:3  4  5  6-tetrafluorophthalic acid  synthesis  optimization
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