Automated radiosynthesis of [¹¹ C]UCB-J for imaging synaptic density by positron emission tomography

An automated radiosynthesis of carbon-11 positron emission tomography radiotracer [¹¹ C]UCB-J for imaging the synaptic density biomarker synaptic vesicle glycoprotein SV2A was established using Synthra RNPlus synthesizer. Commercially available trifluoroborate UCB-J analogue was used as a radiolabelling precursor, and the desired radiolabelled product was isolated in 11 ± 2% (n = 7) nondecay corrected radiochemical yield and formulated as a 10% EtOH solution in saline with molar activities of 20 to 100 GBq/micromol. The method was based upon the palladium(0)-mediated Suzuki cross-coupling reaction and [¹¹ C]CH₃ I as a radiolabelling synthon. The isolated product was cGMP compliant as demonstrated by the results of quality control analysis.