Synthesis of [18F]GBR13119, a presynaptic dopamine uptake antagonist.

[18F]GBR13119 (1-[(4-[18F]fluorophenyl)-(phenyl)methoxy]ethyl-4-(3-phenylpropyl) piperazine) has been prepared in no carrier added form by a four-step synthesis from [18F]fluoride. Isolated yields are 7-10% (uncorrected) in a synthesis time of 120 min. The product is obtained in high specific activity (greater than 1000 Ci/mmol) and high radiochemical purity (greater than 99%) without chromatographic purification. Small amounts of chemical impurity, identified as the nitro-substituted analog by independent synthesis, can be removed by HPLC. [18F]GBR13119 is proposed as a new radiotracer for the presynaptic dopamine uptake system.