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A new iodo tetrazine (Tz) derivative has been synthesized and further developed into the corresponding iodine\u2010125 (<jats:sup>125<\/jats:sup>I) analog (<jats:bold>12<\/jats:bold>), via the trimethylstannane precursor. Radiolabeling with either <jats:italic>N<\/jats:italic>\u2010chlorosuccinimide or chloramine\u2010T, in either MeCN or MeOH proceeded with a radiochemical conversion (RCC) of &gt;80%. Subsequent deprotection only proved successful, among the tested conditions, when the radiolabeled Tz was stirred in 6\u2010M HCl<jats:sub>(aq.)<\/jats:sub> at 60\u00b0C for 2.5\u00a0h. To the best of our knowledge, this is the first H\u2010tetrazine labeled with iodine. In vivo investigations on the pretargeting ability of <jats:bold>12<\/jats:bold> are currently under way.<\/jats:p>","DOI":"10.1002\/jlcr.4009","type":"journal-article","created":{"date-parts":[[2022,12,20]],"date-time":"2022-12-20T23:12:35Z","timestamp":1671577955000},"page":"22-30","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Synthesis and radiolabeling of a polar [<sup>125<\/sup>I]I\u20101,2,4,5\u2010tetrazine"],"prefix":"10.1002","volume":"66","author":[{"given":"Natasha","family":"Bidesi","sequence":"first","affiliation":[{"name":"Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences University of Copenhagen  Copenhagen Denmark"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Vladimir","family":"Shalgunov","sequence":"additional","affiliation":[{"name":"Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences University of Copenhagen  Copenhagen Denmark"},{"name":"Department of Clinical Physiology, Nuclear Medicine and PET Rigshospitalet  Copenhagen Denmark"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1012-8644","authenticated-orcid":false,"given":"Umberto Maria","family":"Battisti","sequence":"additional","affiliation":[{"name":"Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences University of Copenhagen  Copenhagen Denmark"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lars","family":"Hvass","sequence":"additional","affiliation":[{"name":"Department of Clinical Physiology, Nuclear Medicine and PET &amp; Cluster for Molecular Imaging, Copenhagen University Hospital \u2013 Rigshospitalet &amp; Department of Biomedical Sciences University of Copenhagen  Copenhagen Denmark"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jesper Tranekj\u00e6r","family":"J\u00f8rgensen","sequence":"additional","affiliation":[{"name":"Department of Clinical Physiology, Nuclear Medicine and PET &amp; Cluster for Molecular Imaging, Copenhagen University Hospital \u2013 Rigshospitalet &amp; Department of Biomedical Sciences University of Copenhagen  Copenhagen Denmark"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Christian B. 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