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高等学校化学研究 ›› 2011, Vol. 27 ›› Issue (6): 981-983.

• Articles • 上一篇    下一篇

New Way to Synthesize DW286―a Novel Fluoronaphthyridone Antibacterial Agent

FENG Lian-shun, LIU Ming-liang*, ZHANG Yi-bin and GUO Hui-yuan   

  1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, P. R. China
  • 收稿日期:2010-12-06 修回日期:2011-04-27 出版日期:2011-11-25 发布日期:2011-11-07
  • 通讯作者: LIU Ming-liang E-mail:lmllyx@yahoo.com.cn
  • 基金资助:

    Supported by the National S&T Major Special Project of China on Major New Drug Innovation(No.2009ZX09301-003).

New Way to Synthesize DW286―a Novel Fluoronaphthyridone Antibacterial Agent

FENG Lian-shun, LIU Ming-liang*, ZHANG Yi-bin and GUO Hui-yuan   

  1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, P. R. China
  • Received:2010-12-06 Revised:2011-04-27 Online:2011-11-25 Published:2011-11-07
  • Contact: LIU Ming-liang E-mail:lmllyx@yahoo.com.cn
  • Supported by:

    Supported by the National S&T Major Special Project of China on Major New Drug Innovation(No.2009ZX09301-003).

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摘要： A new route for the synthesis of DW286, 7-[3-(aminomethyl)-4-(methoxyimino)-3-methyltetrahy- dro-1H-1-pyrrolyl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid hydrochloric acid salt, is described. In the presence of benzadehyde, DW286 was prepared by the direct condensation of 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid with new pyrrolidine derivative 7 which could be obtained by routine reactions.

关键词: DW286, Benzadehyde, Direct condensation

Abstract: A new route for the synthesis of DW286, 7-[3-(aminomethyl)-4-(methoxyimino)-3-methyltetrahy- dro-1H-1-pyrrolyl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid hydrochloric acid salt, is described. In the presence of benzadehyde, DW286 was prepared by the direct condensation of 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid with new pyrrolidine derivative 7 which could be obtained by routine reactions.

Key words: DW286, Benzadehyde, Direct condensation