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司氟沙星合成新工艺研究 被引量:2

Study on new process of synthesizing sparfloxacin
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摘要 目的:合成氟喹诺酮类抗菌药司氟沙星。方法:以2,3,4,5-四氟苯甲酸为原料,经硝化、酰氯化后与N,N-二甲氨基丙烯酸乙酯偶联,再经环丙胺取代、催化环合、硝基还原、酸性水解等反应,最后与顺式-2,6-二甲基哌嗪缩合。结果与结论:该法缩短了工艺流程,反应条件温和,三废减少,收率有所提高(总收率为34.2%),有较好的工业应用前景。 Objective: To study a new process for preparing the fluoroquinolone antibacterial drug sparfloxacin. Methods: The objective compound was prepared from 2,3,4,5-tetrafluorobenzoic acid, via nitration and acyl chlorination before coupling with ethyl N,N-dimethylamino- acrylate, cyclopropylamine displacement, cyclization, reduction, hydrolysis, and then condensation with 2,6-dimethylpiperazine. Result and Conclusion: The total yield was 34.2% of the input. Different from the old process, the new one can curtail three reaction steps;diethyl malonate condensation, partial hydrolysis decarboxylation, and triethylorthoformate condensation. The new process has many advantages, including short reaction period, mild reaction condition, waste reduction, yield increase, with a good prospect for industrial application.
出处 《中国新药杂志》 CAS CSCD 北大核心 2008年第9期757-759,共3页 Chinese Journal of New Drugs
关键词 司氟沙星 氟喹诺酮 N N-二甲氨基丙烯酸乙酯 合成 sparfloxacin fluoroquinolone ethyl N, N-dimethylaminoacrylate synthesis
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