Rapid and efficient synthesis of high-purity fluorine-18 labeled haloperidol and spiperone via the nitro precursor in combination with a new HPLC separation method

Article abstract of DOI:10.1246/bcsj.70.681

We have completed a convenient synthesis of fluorine-18 labeled butyrophenone neuroleptics from their nitro precursors. Thus, we have developed an efficient single-columm HPLC system using a C₁₈-bonded vinyl alcohol copolymer gel (octadecyl polymer, ODP) column and strongly alkaline solvent systems for purifying of the ¹⁸F-labeled butyrophenone neuroleptics obtained by a single-stp ¹⁸F-for-nitro exchange reaction. The method has been applied to the synthesis of two typical butyrophenone neuroleptics ([¹⁸F]haloperidol and [¹⁸F]spiperone) with high purity in high yield. With information concerning the optimized conditions for the ¹⁸F-for-nitro exchange reaction, the synthetic method would be useful for synthesizing various ¹⁸F-labeled compounds.