{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,24]],"date-time":"2026-09-24T07:52:59Z","timestamp":1790236379946,"version":"4.1.0"},"reference-count":28,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2020,4,28]],"date-time":"2020-04-28T00:00:00Z","timestamp":1588032000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["analyticalsciencejournals.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Labelled Comp Radiopharmac"],"published-print":{"date-parts":[[2020,6,30]]},"abstract":"<jats:p>L\u20102\u2010[<jats:sup>18<\/jats:sup>F]fluoro\u2010alpha\u2010methylphenylalanine (2\u2010[<jats:sup>18<\/jats:sup>F]FAMP) is a promising amino acid tracer for positron emission tomography (PET) imaging, yet the low production yield of direct electrophilic radiofluorination with [<jats:sup>18<\/jats:sup>F]F<jats:sub>2<\/jats:sub> necessitates further optimization of the radiolabeling process. This paper describes a two\u2010step preparation method for L\u20102\u2010[<jats:sup>18<\/jats:sup>F]fluoro\u2010alpha\u2010methylphenylalanine (2\u2010[<jats:sup>18<\/jats:sup>F]FAMP) starting from [<jats:sup>18<\/jats:sup>F]fluoride. The (Mesityl)(L\u2010alpha\u2010methylphenylalanine)\u20102\u2010iodonium tetrafluoroborate precursors with various protecting groups were prepared. The copper\u2010mediated <jats:sup>18<\/jats:sup>F\u2010fluorination of the iodonium salt precursors successfully produced 2\u2010[<jats:sup>18<\/jats:sup>F]FAMP. The highest radio chemical conversion of 57.6% was noted with <jats:italic>N<\/jats:italic>\u2010Piv\u2010protected (mesityl)(aryl)iodonium salt in the presence of 5 equivalent of Cu (OTf)<jats:sub>2<\/jats:sub>. Subsequent deprotection with 57% hydrogen iodide produced 2\u2010[<jats:sup>18<\/jats:sup>F]FAMP within 120 min in 21.4 \u00b1 11.7% overall radiochemical yield with &gt;95% radiochemical purity and an enantiomeric excess &gt;99%. The obtained 2\u2010[<jats:sup>18<\/jats:sup>F]FAMP showed comparable biodistribution profiles in normal mice with that of the carrier\u2010added 2\u2010[<jats:sup>18<\/jats:sup>F]FAMP. These results indicate that usefulness of copper mediated <jats:sup>18<\/jats:sup>F\u2010fluorination for the production of 2\u2010[<jats:sup>18<\/jats:sup>F]FAMP, which would facilitate clinical translation of the promising tumor specific amino acid tracer. Individual facilities could adopt either production method based on radioactivity demand and equipment availability.<\/jats:p>","DOI":"10.1002\/jlcr.3840","type":"journal-article","created":{"date-parts":[[2020,3,28]],"date-time":"2020-03-28T02:00:58Z","timestamp":1585360858000},"page":"368-375","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Selective synthesis of L\u20102\u2010[<sup>18<\/sup>F]fluoro\u2010alpha\u2010methylphenylalanine via copper\u2010mediated <sup>18<\/sup>F\u2010fluorination of (mesityl)(aryl)iodonium salt"],"prefix":"10.1002","volume":"63","author":[{"given":"Aiko","family":"Yamaguchi","sequence":"first","affiliation":[{"name":"Bioimaging Information Analysis Gunma University Graduate School of Medicine  Maebashi Japan"},{"name":"Texas Therapeutics Institute, The Brown Foundation Institute of Molecular Medicine The University of Texas Health Science Center at Houston  Houston Texas 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