Monaco, Alessandra Michelin, Olivier Prior, John Rüegg, Curzio Scapozza, Leonardo Seimbille, Yann 2014-03-01 Arginine–glycine–aspartic acid (RGD)-containing peptides have been traditionally used as PET probes to noninvasively image angiogenesis, but recently, small selective molecules for <em>α</em>₅<em>β</em>₁ integrin receptor have been developed with promising results. Sixty-one antagonists were screened, and <em>tert</em>-butyl (S)-3-(2-((3R,5S)-1-(3-(1-(2-fluoroethyl)-1H-1,2,3-triazol-4- yl)propanoyl)-5-((pyridin-2-ylamino)methyl)pyrrolidin-3-yloxy)acetamido)-2-(2,4,6- trimethylbenzamido)propanoate (FPMt) was selected for the development of a PET tracer to image the expression of <em>α</em>₅<em>β</em>₁ integrin receptors. An alkynyl precursor (PMt) was initially synthesized in six steps, and its radiolabeling was performed according to the azide–alkyne copper(II)-catalyzed Huisgen's cycloaddition by using 1-azido-2-[¹⁸F]fluoroethane ([¹⁸F]12). Different reaction conditions between PMt and [¹⁸F]12 were investigated, but all of them afforded [¹⁸F]FPMt in 15 min with similar radiochemical yields (80–83%, decay corrected). Overall, the final radiopharmaceutical ([¹⁸F]FPMt) was obtained after a synthesis time of 60–70 min in 42–44% decay-corrected radiochemical yield. application/pdf https://folia.unifr.ch/global/documents/303628 https://folia.unifr.ch/documents/303628/files/rue_snp.pdf eng info:eu-repo/semantics/altIdentifier/doi/10.1002/jlcr.3190 info:eu-repo/semantics/openAccess License undefined Journal of labelled compounds & radiopharmaceuticals. - 2014, vol. 57, no. 5, p. 365-370 <em>α</em>₅<em>β</em>₁ integrin receptor PET, 1-azide-2-[¹⁸F]fluoroethane click chemistry peptido-mimetic info:eu-repo/classification/udc/57 Synthesis of a non-peptidic PET tracer designed for α5β1 integrin receptor http://purl.org/coar/resource_type/c_6501