Synthesis of [11C]levofloxacin
Abstract
Abstract 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.
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