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Meanwhile, safinamide shows tremendous therapeutic potential in the context of other central nervous system diseases (e.\u2009g. ischaemic stroke, amyotrophic lateral sclerosis, depression, etc.). In this work, [<jats:sup>18<\/jats:sup>F]safinamide, which is safinamide labelled by the positron\u2010emitting radionuclide [<jats:sup>18<\/jats:sup>F]fluorine, was synthesized automatically based on iodonium ylide precursors with high radiochemical yield and high molar activity. Density functional theory was applied to calculate the Gibbs free energy change during iodonium ylide\u2010mediated fluorination and to interpret the effect of tetraethylammonium (TEA<jats:sup>+<\/jats:sup>) as the counter cation in these reactions to improve the nucleophilicity of [<jats:sup>18<\/jats:sup>F\/<jats:sup>19<\/jats:sup>F]fluoride. In addition, positron emission tomography studies on Sprague Dawley rats were carried out to determine the imaging characteristics, pharmacokinetics, and metabolism of the [<jats:sup>18<\/jats:sup>F]safinamide radiotracer. The results displayed the complete biodistribution of the radiotracer, especially in rat brains, and revealed that [<jats:sup>18<\/jats:sup>F]safinamide has moderate brain uptake, rapid and reversible binding kinetics, and good stability.<\/jats:p>","DOI":"10.1002\/cmdc.202200472","type":"journal-article","created":{"date-parts":[[2022,9,7]],"date-time":"2022-09-07T01:51:05Z","timestamp":1662515465000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Highly Efficient Radiosynthesis and Biological Evaluation of [<sup>18<\/sup>F]Safinamide, a Radiolabelled Anti\u2010Parkinsonian Drug for Positron Emission Tomography Imaging"],"prefix":"10.1002","volume":"17","author":[{"given":"Yangyang","family":"Xu","sequence":"first","affiliation":[{"name":"College of Chemical &amp; Biological Engineering Zhejiang University Hangzhou  Zhejiang 310027 P.R. 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