Synthesis of [11C]levofloxacin

Synthesis of [11C]levofloxacin

Levofloxacin, the pure S enantiomer of the fluoroquinolone antibiotic ofloxacin, was labeled via methylation of the corresponding, des‐methyl, secondary amine with N.C.A. [11C]methyl iodide. The methylation reaction was regioselective, giving predominantly the preferred methyl amine at high temperat...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 2001-10, Vol.44 (12), p.859-864
Hauptverfasser: Berridge, M. S., Burnazi, E. M.
Format: Artikel
Sprache:eng
Schlagworte:
antibiotic
carbon-11
Chemistry
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms
levofloxacin
methyl iodide
Organic chemistry
Preparations and properties
regioselective
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Beschreibung
Zusammenfassung:Levofloxacin, the pure S enantiomer of the fluoroquinolone antibiotic ofloxacin, was labeled via methylation of the corresponding, des‐methyl, secondary amine with N.C.A. [11C]methyl iodide. The methylation reaction was regioselective, giving predominantly the preferred methyl amine at high temperature in DMF, while otherwise giving predominantly the methyl ester of a free carboxylic acid also present in the molecule. Levofloxacin was obtained in 80% chemical yield after a 45 min synthesis. Copyright © 2001 John Wiley & Sons, Ltd.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.510