Fully automated radiosynthesis of [ 18 F]fluoro- C -glyco-c(RGDfC): exploiting all the abilities of the AllInOne synthesizer

Radiolabelled peptides are crucial tools for biomedical research purposes. Peptides are usually labeled with fluorine-18 via an indirect prosthetic group approach, which requires a complex multistep procedure not easily automatable. However, automation is a compulsory step of paramount importance to...

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Veröffentlicht in:Reaction chemistry & engineering 2019-12, Vol.4 (12), p.2088-2098
Hauptverfasser: Collet, Charlotte, Vucko, Timothé, Ariztia, Julen, Karcher, Gilles, Pellegrini-Moïse, Nadia, Lamandé-Langle, Sandrine
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Sprache:eng
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Zusammenfassung:Radiolabelled peptides are crucial tools for biomedical research purposes. Peptides are usually labeled with fluorine-18 via an indirect prosthetic group approach, which requires a complex multistep procedure not easily automatable. However, automation is a compulsory step of paramount importance to produce radiotracers with high reliability and minimal human involvement. Herein, we describe the fully automated radiosynthesis of [ 18 F]fluoro- C -glyco-c(RDGfC) on an AllInOne (AIO) synthesizer, exploiting for the first time all the abilities of the AIO module. The radiotracer was prepared in high radiochemical purity via a challenging three-step sequence in 140 minutes with a decay-corrected radiochemical yield of 3.6 ± 0.4%. Presenting a high stability and an improved hydrophilicity, [ 18 F]fluoro- C -glyco-c(RDGfC) could become a valuable tool in PET imaging for cancer diagnosis. Furthermore, the described automated procedure is modular and could be adapted to other prosthetic groups and/or peptides with minimal changes to afford a large panel of 18 F-radiolabeled peptides.
ISSN:2058-9883
2058-9883
DOI:10.1039/C9RE00303G