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《Journal of Chemical Engineering of Chinese Universities》 2005-05
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Study on New Process of Synthesizing Levofloxacin

GU Hai-ning1, JIANG Yong-xiang2, GE Hai-quan 3 (1. Center of Analysis & Measurement of Zhejiang University, Hangzhou 310028, China; 2. Huzhou Entry-Exit Inspection and Quarantine Bureau, Huzhou 313000, China; 3.Hangzhou Great Froest Biomedical Co. Ltd., Hangzhou 310028, China)  
New process for preparing the fluoroquinolone antibacterial drug levofloxacin was described. The object compound was prepared from 2,3,4,5-tetrafluorobenzoic acid, via acyl chlorination, ethyl N,N-dimethylaminoacrylate coupling, S-(+)-2-aminopropanol displacement, cyclization, hydrolysis, and finally N-methylpiperazine condesation, the total yield is 52.3%. Comparing to the old process conventionally used at present, the application of the new starting material ethyl N, N-dimethylaminoacrylate can curtail three reaction steps, they are the diethyl malonate condensation, partial hydrolysis decarboxylation and triethylorthoformate condensation. New process has many advantages, such as simple procedure, short reaction period, high optical purity, cheaper raw material,higher yield. So it should have a good prospect for industrial application.
【CateGory Index】: TQ463.53
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