{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T05:00:58Z","timestamp":1787029258119,"version":"build-2736575974"},"reference-count":44,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2024,12,20]],"date-time":"2024-12-20T00:00:00Z","timestamp":1734652800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"the state assignment of the Ministry of Education and Science of Russian Federation","award":["FMMW-2022-0006"],"award-info":[{"award-number":["FMMW-2022-0006"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>Background:\u00a0N-succinimidyl-[18F]fluorobenzoate ([18F]SFB) is commonly prepared through a three-step procedure starting from [18F]fluoride ion. A number of methods for the single-step radiosynthesis of [18F]SFB have been introduced recently, including the radiofluorination of diaryliodonium salts and the Cu-mediated 18F-fluorination of pinacol aryl boronates and aryl tributyl stannanes, but they still have the drawbacks of lengthy product purification procedures. In the present work, two approaches for the direct labeling of [18F]SFB from diaryliodonium (DAI) salt (4) and pinacol aryl boronate (6) are evaluated, with a major focus on developing a fast and simple SPE-based purification procedure. Methods: DAI salt precursor 6 was labeled employing the common \u201cminimalist\u201d approach with a two-step reaction heating sequence. The Cu-mediated radiofluorination of 4 was accomplished using Bu4NOTf as a phase transfer catalyst for the elution of [18F]fluoride, followed by radiofluorination in the same solvent. Several types of SPE cartridges were tested in the elution and SPE procedures. Results: The Cu-mediated 18F-fluorination of the pinacol aryl boronate precursor afforded a higher RCC of 56 \u00b1 3% (n = 7), making it better suited for the one-pot synthesis of [18F]SFB. SPE-based purification was achieved using cation exchange and reverse-phase polymer resin cartridges, connected in series. In a full-batch test, [18F]SFB was obtained with an RCY of 30% (n. d. c.), RCP &gt; 99%, Am 96\u2013155 GBq\/\u00b5mol, and a synthesis time of \u226435 min. Conclusions: Compared to other published methods, [18F]SFB production via the Cu-mediated radiofluorination of pinacol aryl boronate precursor provides significant time and cost savings, coupled with an ease of implementation.<\/jats:p>","DOI":"10.3390\/ph17121723","type":"journal-article","created":{"date-parts":[[2024,12,20]],"date-time":"2024-12-20T06:44:33Z","timestamp":1734677073000},"page":"1723","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["Simple and Efficient Synthesis of N-Succinimidyl-4-[18F]fluorobenzoate ([18F]SFB)\u2014An Important Intermediate for the Introduction of Fluorine-18 into Complex Bioactive Compounds"],"prefix":"10.3390","volume":"17","author":[{"given":"Viktoriya V.","family":"Orlovskaya","sequence":"first","affiliation":[{"name":"N. P. Bechtereva Institute of the Human Brain, Russian Academy of Sciences, 197022 St. Petersburg, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Olga S.","family":"Fedorova","sequence":"additional","affiliation":[{"name":"N. P. Bechtereva Institute of the Human Brain, Russian Academy of Sciences, 197022 St. Petersburg, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8369-2537","authenticated-orcid":false,"given":"Nikolai B.","family":"Viktorov","sequence":"additional","affiliation":[{"name":"Faculty of Chemical and Biotechnology, St. Petersburg State Institute of Technology (Technical University), 190013 St. Petersburg, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4201-7949","authenticated-orcid":false,"given":"Raisa N.","family":"Krasikova","sequence":"additional","affiliation":[{"name":"N. P. Bechtereva Institute of the Human Brain, Russian Academy of Sciences, 197022 St. Petersburg, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2024,12,20]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"615","DOI":"10.1021\/cbmi.4c00030","article-title":"Peptide PET Imaging: A Review of Recent Developments and a Look at the Future of Radiometal-Labeled Peptides in Medicine","volume":"2","author":"Shabsigh","year":"2024","journal-title":"Chem. Biomed. 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