加替沙星合成工艺改进研究  

Process Imporvement of Synthesis of Gatifloxacin

作　　者：李倩[1] 赵世明[2] 罗振福[2] 孙有光[1] 

机构地区：[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

出　　处：《精细化工中间体》2009年第5期37-40,69,共5页Fine Chemical Intermediates

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。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.

关 键 词：3 4 5 6-四氟苯二甲酸 合成 优化 

分 类 号：TQ253.2[化学工程—有机化工]