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Article Navigation> JOURNAL OF BEIJING INSTITUTE OF TECHNOLOGY> 2013> 22(1): 130-134
FU Yan-jie, SUN Li-quan, FAN Xin-yuan, LIU Cong, YAO Guo-wei, LUO Ai-qin. Improvement in synthesis of 3'-N-demethylazithromycin and its derivatives[J]. JOURNAL OF BEIJING INSTITUTE OF TECHNOLOGY, 2013, 22(1): 130-134.
Citation: FU Yan-jie, SUN Li-quan, FAN Xin-yuan, LIU Cong, YAO Guo-wei, LUO Ai-qin. Improvement in synthesis of 3'-N-demethylazithromycin and its derivatives[J].JOURNAL OF BEIJING INSTITUTE OF TECHNOLOGY, 2013, 22(1): 130-134.
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Improvement in synthesis of 3'-N-demethylazithromycin and its derivatives

  • School of Life Science, Beijing Institute of Technology, Beijing 100081, China

  • Received Date:2012-04-20
    Abstract
  • 3'- N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethylation of azithromycin, i.e., azithromycin loses a methyl group on the 3'- Nposition. In this study, bulk product was purified with chromatographic separation. It was observed that 3'- N-demethylazithromycin was also a precursor of other impurities. Simultaneously, another derivative was synthesized, i.e., 3'- N-demethyl-3'- N-formylazithromycin. Reaction conditions were optimized with the HPLC method and good-quality and high-yield derivative product was achieved. The structures of derivatives were identified by 1H-NMR and MS.
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