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

• Published in: Reaction chemistry & engineering Vol. 4; no. 12; pp. 288 - 298
• Main Authors: Collet, Charlotte, Vucko, Timothé, Ariztia, Julen, Karcher, Gilles, Pellegrini-Moïse, Nadia, Lamandé-Langle, Sandrine
• Format: Journal Article
• Language: English
• Published: 19.11.2019
• ISSN: 2058-9883
• DOI: 10.1039/c9re00303g

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. Fully automated and modular radiosynthesis of [ 18 F]fluoro- C -glyco-RGD conjugate.