Study on direct electrophilic radiofluorination of amino acid derivatives

Objective To study an easy and fast method for the radiofluorination of amino acid derivatives.Methods The radiosynthesis procedure was divided into 3 steps:(1) Synthesis of ¹⁸F₂gas by ²⁰Ne (d,α)¹⁸F reaction in cyclotron. (2) By passing through a specific column, ¹⁸F₂ gas was converted into CH₃COO¹⁸F. (3) Fluorinated amino acid derivatives were synthesized by direct electrophilic reaction between amino acids and CH₃COO¹⁸F.Results It took about 45 minutes to fulfill the whole synthesis procedure. The radioactivity yield rate, radiochemistry purity and pH value was about 60%, >95% and about 7 respectively. Both sterility and apyrogenicity test showed negative result. All these results guaranteed the following animal study and clinical application.Conclusion It is suggested that electrophilic radiofluorination reaction is an easy and fast way for the radiolabeling of amino acid derivatives.