Synthesis and murine tissue uptake of sodium [18F]fluoroacetate

Fluoroacetate (FAc) is well known as the rodenticide "1080" and for its potent biochemical properties, but much less is known about its behavior in vivo. In order to study this behavior, the compound was labeled with 18F. The synthesis was accomplished in good yields (30%) from carrier-added radiofluorine gas by its conversion to [18F]tetrabutylammonium fluoride, followed by a heat-assisted halogen exchange with ethylbromoacetate. The isolated ester was rapidly and quantitatively hydrolysed with base to form [18F]FAc. preliminary studies in mice revealed relatively little soft tissue retention over the 4 h study period. However, substantial bone accumulation, indicative of defluorination, occurred to a significant degree.