{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,17]],"date-time":"2025-10-17T00:35:33Z","timestamp":1760661333411,"version":"build-2065373602"},"reference-count":17,"publisher":"Wiley","issue":"5-6","license":[{"start":{"date-parts":[[2025,5,5]],"date-time":"2025-05-05T00:00:00Z","timestamp":1746403200000},"content-version":"vor","delay-in-days":4,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/100009619","name":"Japan Agency for Medical Research and Development","doi-asserted-by":"publisher","award":["JP22dm0207092"],"award-info":[{"award-number":["JP22dm0207092"]}],"id":[{"id":"10.13039\/100009619","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["analyticalsciencejournals.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Labelled Comp Radiopharmac"],"published-print":{"date-parts":[[2025,5]]},"abstract":"<jats:title>ABSTRACT<\/jats:title><jats:p>Animal models of Alzheimer's disease (<jats:sc>AD<\/jats:sc>) are essential for developing therapeutics and evaluating the efficacy of new drug candidates. Positron emission tomography (PET) is a useful method to monitor a major hallmark of the onset of <jats:sc>AD<\/jats:sc>, namely, the deposition of amyloid \u03b2 peptide (A\u03b2) in the brain. [<jats:sup>18<\/jats:sup>F]FC\u2010119S (<jats:bold>1<\/jats:bold>), a 2\u2010pyridylbenzothiazole analog, has been applied as a radiotracer for PET visualization of A\u03b2 plaques in an <jats:sc>AD<\/jats:sc> model, the 5xFAD mouse. Here, we present an alternative method for the automated synthesis of <jats:sup>18<\/jats:sup>F\u2010labeled <jats:bold>1<\/jats:bold> as a radiotracer for our animal PET studies. The first attempt at synthesizing <jats:sup>18<\/jats:sup>F\u2010labeled <jats:bold>1<\/jats:bold> using a mesyl precursor afforded desired product <jats:bold>1<\/jats:bold>, although a nonfluorinated mesyl byproduct was eluted prior to <jats:bold>1<\/jats:bold> during purification by semipreparative high\u2010performance liquid chromatography. An alternative synthesis using a tosyl precursor was applied to delay the elution of a nonfluorinated byproduct during chromatographic purification. As a result, <jats:sup>18<\/jats:sup>F\u2010labeled <jats:bold>1<\/jats:bold> was eluted without proximate byproducts during chromatographic purification, and routine production of <jats:sup>18<\/jats:sup>F\u2010labeled <jats:bold>1<\/jats:bold> was achieved for our <jats:sc>AD<\/jats:sc> studies using animal models.<\/jats:p>","DOI":"10.1002\/jlcr.4145","type":"journal-article","created":{"date-parts":[[2025,5,5]],"date-time":"2025-05-05T11:18:19Z","timestamp":1746443899000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Synthesis of <sup>18<\/sup>F\u2010Labeled FC\u2010119S and Its Tosyl Precursor"],"prefix":"10.1002","volume":"68","author":[{"ORCID":"https:\/\/orcid.org\/0009-0003-1894-7905","authenticated-orcid":false,"given":"Koichi","family":"Kato","sequence":"first","affiliation":[{"name":"Division of Radiation Protection, National Institute of Neuroscience National Center of Neurology and Psychiatry  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Makoto","family":"Funasaka","sequence":"additional","affiliation":[{"name":"Department of Neurophysiology, National Institute of Neuroscience National Center of Neurology and Psychiatry  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jun","family":"Ogura","sequence":"additional","affiliation":[{"name":"Department of Neurophysiology, National Institute of Neuroscience National Center of Neurology and Psychiatry  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eiko\u00a0N.","family":"Minakawa","sequence":"additional","affiliation":[{"name":"Department of Neurophysiology, National Institute of Neuroscience National Center of Neurology and Psychiatry  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kazuhiko","family":"Seki","sequence":"additional","affiliation":[{"name":"Department of Neurophysiology, National Institute of Neuroscience National Center of Neurology and Psychiatry  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Takuya","family":"Kumamoto","sequence":"additional","affiliation":[{"name":"Department of Synthetic Organic Chemistry, Graduate School of Biomedical and Health Sciences Hiroshima University  Hiroshima Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2025,5,5]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.1111\/jnc.13632"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.15252\/emmm.201606210"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1002\/jlcr.2989"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.3389\/fnins.2022.807473"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.neuron.2019.07.010"},{"key":"e_1_2_8_7_1","doi-asserted-by":"publisher","DOI":"10.3389\/fnagi.2014.00235"},{"key":"e_1_2_8_8_1","doi-asserted-by":"publisher","DOI":"10.1523\/JNEUROSCI.1907-16.2016"},{"key":"e_1_2_8_9_1","doi-asserted-by":"publisher","DOI":"10.1523\/JNEUROSCI.0673-07.2007"},{"key":"e_1_2_8_10_1","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pone.0031310"},{"key":"e_1_2_8_11_1","doi-asserted-by":"publisher","DOI":"10.2967\/jnumed.112.110163"},{"key":"e_1_2_8_12_1","doi-asserted-by":"publisher","DOI":"10.1186\/s12868-018-0447-7"},{"key":"e_1_2_8_13_1","doi-asserted-by":"publisher","DOI":"10.2967\/jnumed.119.227322"},{"key":"e_1_2_8_14_1","article-title":"Early Detection of A\u03b2 Deposition in the 5xFAD Mouse by Amyloid PET","author":"Oh S. J.","year":"2018","journal-title":"Contrast Media & Molecular Imaging"},{"key":"e_1_2_8_15_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2016.03.034"},{"key":"e_1_2_8_16_1","doi-asserted-by":"publisher","DOI":"10.1021\/ja0646895"},{"key":"e_1_2_8_17_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0040-4020(01)96443-9"},{"key":"e_1_2_8_18_1","unstructured":"\u201cAnimal PET Studies Using 6 Months Old 5xFAD Mice as Tg Model and Their Age\u2010Matched Littermates as WT Were Performed and Around 30% Increment in the SUV Was Observed for the Hippocampus and Thalamus of Tg Mouse as Compared to WT. These Results are Correlated Well With Previous Report [13].\u201d"}],"container-title":["Journal of Labelled Compounds and Radiopharmaceuticals"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/analyticalsciencejournals.onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/jlcr.4145","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,16]],"date-time":"2025-10-16T18:52:30Z","timestamp":1760640750000},"score":1,"resource":{"primary":{"URL":"https:\/\/analyticalsciencejournals.onlinelibrary.wiley.com\/doi\/10.1002\/jlcr.4145"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,5]]},"references-count":17,"journal-issue":{"issue":"5-6","published-print":{"date-parts":[[2025,5]]}},"alternative-id":["10.1002\/jlcr.4145"],"URL":"https:\/\/doi.org\/10.1002\/jlcr.4145","archive":["Portico"],"relation":{},"ISSN":["0362-4803","1099-1344"],"issn-type":[{"type":"print","value":"0362-4803"},{"type":"electronic","value":"1099-1344"}],"subject":[],"published":{"date-parts":[[2025,5]]},"assertion":[{"value":"2025-01-28","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2025-04-08","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2025-05-05","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}],"article-number":"e4145"}}