Enabling Efficient Positron Emission Tomography (PET) Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) with a Robust and One-Step Radiosynthesis of a Highly Potent ¹⁸F‑Labeled Ligand ([¹⁸F]UCB-H)

We herein describe the straightforward synthesis of a stable pyridyl­(4-methoxyphenyl)­iodonium salt and its [¹⁸F] radiolabeling within a one-step, fully automated and cGMP compliant radiosynthesis of [¹⁸F]­UCB-H ([¹⁸F]<b>7</b>), a PET tracer for the imaging of synaptic vesicle glycoprotein 2A (SV2A). Over the course of 1 year, 50 automated productions provided 34 ± 2% of injectable [¹⁸F]<b>7</b> from up to 285 GBq (7.7 Ci) of [¹⁸F]­fluoride in 50 min (uncorrected radiochemical yield, specific activity of 815 ± 185 GBq/μmol). The successful implementation of our synthetic strategy within routine, high-activity, and cGMP productions attests to its practicality and reliability for the production of large doses of [¹⁸F]<b>7</b>. In addition to enabling efficient and cost-effective clinical research on a range of neurological pathologies through the imaging of SV2A, this work further demonstrates the real value of iodonium salts for the cGMP ¹⁸F-PET tracer manufacturing industry, and their ability to fulfill practical and regulatory requirements in that field