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A large variety of PSMA ligands have been radiolabeled, to date. Among the various derivatives, PSMA\u2010617 resulted to be one of the most interesting in terms of interaction with the antigen and clinical properties, and its lutetium\u2010177 labeled version has recently been approved by regulatory agencies for therapeutic purposes. For this reasons, the radiolabeling with fluorine\u201018 of a PSMA\u2010617 derivative might be of interest. Beside other methodologies to radiolabel macromolecules with fluorine\u201018, the \u201cclick\u2010chemistry\u201d approach resulted to be very useful, and the copper\u2010catalyzed azide\u2010alkyne cycloaddition (CuAAC) is considered one of most efficient and reliable. This paper proposes the synthesis of a suitable precursor for the radiolabeling with fluorine\u201018 of a new PSMA\u2010617 derivative. The whole radiosynthetic procedure has been fully automated, and the final product, which proved to be stable in plasma, has been obtained with radiochemical yield and purity suitable for subsequent preclinical studies.<\/jats:p>","DOI":"10.1002\/jlcr.3959","type":"journal-article","created":{"date-parts":[[2021,12,28]],"date-time":"2021-12-28T22:28:25Z","timestamp":1640730505000},"page":"48-62","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":9,"title":["Synthesis and automated fluorine\u201018 radiolabeling of new PSMA\u2010617 derivatives with a CuAAC radiosynthetic approach"],"prefix":"10.1002","volume":"65","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-1170-5570","authenticated-orcid":false,"given":"Marco N.","family":"Iannone","sequence":"first","affiliation":[{"name":"Tecnomed Foundation University of Milano\u2010Bicocca  Milan 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