Synthesis of 6-[18F]fluorodopamine, 6-[18F]fluoro-m-tyramine and 4-[18F]fluoro-m-tyramine

Article abstract of DOI:10.1002/jlcr.2580360903

h. new method for the preparation of 6-[¹⁸F]fluorodopamine (3) and [¹⁸F]fluorinated analogs of m-tyramine based on a regioselective radiofluorodestannylation reaction has been developed. The radiofluorodestannylation of 6-trimethylstannyldopamine derivative 1 was carried out with [¹⁸F]F₂ to give the corresponding [¹⁸F]fluoro intermediate 2. Acid deprotection of 2 with 48% HBr followed by HPLC purification afforded 6-[¹⁸F]fluorodopamine (3) in 18% radiochemical yield. Similarly, 6- and 4-[¹⁸F]fluoro-m-tyramines and 6b) were prepared from their corresponding trimethylstannyl-m-tyramine derivatives in 25 and 8% radiochemical yields, respectively. In all cases, after HPLC purification of the final products, tin concentrations were found to be <15 ppb.