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Vol. 26 No. 20 (2014)

Copyright (c) 2014 Yu Liu*, Lianxin Liu, Guangxia Shi

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This work is licensed under a Creative Commons Attribution 4.0 International License.

Synthesis and Characterization of Sitafloxacin

https://doi.org/10.14233/ajchem.2014.17864
Yu Liu*
Xuzhou College of Industrial Technology, Xuzhou 221140, Jiangsu Province, P.R. China *Corresponding author: E-mail: liuyu0138@163.com
Lianxin Liu
Xuzhou College of Industrial Technology, Xuzhou 221140, Jiangsu Province, P.R. China *Corresponding author: E-mail: liuyu0138@163.com
Guangxia Shi
Xuzhou College of Industrial Technology, Xuzhou 221140, Jiangsu Province, P.R. China *Corresponding author: E-mail: liuyu0138@163.com

Corresponding Author(s) : Yu Liu*

Asian Journal of Chemistry, Vol. 26 No. 20 (2014)

Abstract

The convenient protocol for the synthesis of sitafloxacin is described. Reaction of ethyl 3-(3-chloro-2,4,5-trifluorophenyl)-3-oxopropanoate with triethylorthoformate and (1R,2S)-(-)-cis-1,2-fluorine cyclopropane amino-p-toluene sulfonic acid salt by condensation under sodium hydrogen condition. The reaction mixture take place hydrolysis of ester in hydrochloric acid solution. Subsequence reacted with (S)-N-[(oxoboryl)methylene]-5-azaspiro[2,4]heptan-7-amine by condensation. In the end taken off the protection group gives sitafloxacin and total conversion about 52-65 %. The structure of sitafloxacin was characterized by 1H NMR, 13C NMR, IR, MS and elemental analysis.

Keywords

Sitafloxacin Synthesis Characterization.
Liu*, Y., Liu, L., & Shi, G. (2014). Synthesis and Characterization of Sitafloxacin. Asian Journal of Chemistry, 26(20), 7049–7051. https://doi.org/10.14233/ajchem.2014.17864
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