“one-pot” Synthesis of Intermediate of Pazufloxacin
DOI:
CSTR:
Author:
Affiliation:

Clc Number:

Fund Project:

  • Article
  • |
  • Figures
  • |
  • Metrics
  • |
  • Reference
  • |
  • Related
  • |
  • Cited by
  • |
  • Materials
  • |
  • Comments
    Abstract:

    (S)-10-(1-carbamoylcyclopropyl)-9-fluoro-3-methyl-7-oxo-3,7-dihydro-2H -[1,4]-oxazino[2,3,4-ij]quinoline-6-carboxylic acid, the senior intermediate of pazu- floxacin, was synthesiszed from (S)-ethyl 10-(cyanomethyl)-9-fluoro-3-methyl- 7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylate, via a one-pot reaction of cyclopropanation and cyanide hydrolyzation. The reaction conditions were optimized as follows: n (Compound II): n(1,2-dichloroethane): n (Benzyltriethylam monium chloride):n(NaOH) = 1:1.5:0.43:16.7,stirred in water for 5h at room temperature and then reflux for 2h. The method has the advantages of mild reaction condition, safety, low cost, and environmental friendly.

    Reference
    Related
    Cited by
Get Citation
Share
Article Metrics
  • Abstract:
  • PDF:
  • HTML:
  • Cited by:
History
  • Received:October 08,2012
  • Revised:November 30,2012
  • Adopted:December 03,2012
  • Online: January 07,2013
  • Published:
Article QR Code