摘要
从新的三环氟喹诺酮药盐酸芦氟沙星（１）中分离出一种重要杂质，经元素分析、质谱、核磁、红外等鉴定为盐酸氯芦沙星（２），为了进一步确证其结构，合成了该化合物，由２，６－二氯苯胺为起始原料经重氮化、氟化、硝化、缩合、还原、取代、环合、缩合环合、螯合、甲哌化、水解等十三步反应制得盐酸氯芦沙星，该杂质对大肠杆菌、沙门氏菌、克雷伯氏菌等几乎不显示抗菌活性。
An important impurity Cl rufoxacin hydrochloride separated from a new tricyclic fluoroquinolone rufloxacin hydrochloride has been identified and synthesized in thirteen steps from 2,6 dichloroaniline through diazotization, fluoration, nitration, condensation, reduction, substitution, cyclization, condensation cyclization, chelation, N methylpiperazination, and hydrolysis. Cl rufloxacin hydrochloride shows in vitro antibacterial activity insignificantly against E.coli , Salmonella,Klebsiella, etc.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1996年第3期131-135,共5页
Journal of China Pharmaceutical University
关键词
盐酸氯芦沙星
盐酸氯芦沙星
杂质
分离
合成
Cl rufloxacin hydrochloride
Rufloxacin hydrochloride
Separation
Identification
Synthesis
