Direct introduction of a formamido group into the 7.ALPHA.(6.ALPHA.)-position of cephalosporins (pencillins).

DOI

Abstract

A novel direct introduction of a formamido group into the 7α(6α)-position of cephalosporins (penicillins) was achieved by treatment of 7β(6β-[(3, 5-di-tert-butyl-4-oxo-2, 5-cyclohexadien-1-ylidene)methylimino]cephem (penam) esters with N, N-bis(trimethylsilyl)formamide, followed by deblocking with Girard reagent T to give the corresponding 7α(6α)-foimamido-7β(6β-amino derivatives. Three 7α-formamidocephalosporins were prepared by the conventional N-acylation of 7α-formamidocephem. All of them were resistant to β-lactamases, showing similar MIC values against both of a pair of a β-lactamase-producing strain and the corresponding non or low-producing strain of the same species of bacteria, when tested on Staphylococcus aureus, Klebsiella pneurnoniae, Escherichia coli, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Enterobacter cloacae and Citrobacter freundii.

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Keywords

Details 詳細情報について

  • CRID
    1390282679124351872
  • NII Article ID
    130003409955
  • DOI
    10.7164/antibiotics.43.820
  • ISSN
    18811469
    00218820
  • Text Lang
    en
  • Data Source
    • JaLC
    • Crossref
    • CiNii Articles
  • Abstract License Flag
    Disallowed

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