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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 was isolated from the new tricyclic fluoroquinolone rufloxacin hydrochloride (1) and identified as chloraxacin hydrochloride (2) by elemental analysis, mass spectrometry, nuclear magnetic resonance and infrared spectroscopy. In order to confirm its structure, The compound was synthesized from 2,6-dichloroaniline as starting material by diazotization, fluorination, nitration, condensation, reduction, substitution, cyclization, condensation and cyclization, chelation, metropisation, hydrolysis and other ten Three-step reaction of clofloxacin hydrochloride, the impurities of Escherichia coli, Salmonella, Klebsiella etc. showed almost no antibacterial activity.