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兽用氟喹诺酮类药物奥比沙星的合成
陈诚,林渝宁
0
(重庆市畜牧科学院)
摘要:
本文依据现有氟喹诺酮类药物的合成路线和国外奥比沙星的文献报道,以五氟苯甲酰氯为起始物,通过与丙二酸单乙酯钾盐加成、原甲酸三乙酯缩合、与环丙胺取代,然后成环,水解和哌嗪基的取代反应合成出第三代动物专用氟喹诺酮类药物奥比沙星,产物结构经过核磁共振光谱、红外吸收光谱和质谱进行了表征确认。
关键词:  奥比沙星  合成  氟喹诺酮类药物
DOI:
投稿时间:2013-05-27修订日期:2013-08-20
基金项目:重庆市2011年农发资金项目(11404)
Synthesis of Veterinary Fluoroquinolones Orbifloxacin
(ChongQing Academy of Animal Sciences)
Abstract:
A new synthetic method for preparing veterinary fluoroquinolones antimicrobial agents Orbifloxacin which was reported on the basis of the existing synthetic routes of quinolones and its reported on the abroad. Pentafluorobenzoyl chloride was used as a starting material to addition react with ethyl potassium malonate, the condensation of triethyl orthoformate and the substitution reaction with cyclopropylamine. The intermediate was allowed to ring-closure, hydrolysis and substitution reaction of piperazine to yield the desired antibiotics. Orbifloxacin was confirmed by IR、1H NMR and MS spectra.
Key words:  Orbifloxacin  synthesis  fluoroquinolones

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