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 [¹⁸F]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, [¹⁸F]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 ¹⁸F-radiolabeled peptides.

中文翻译：

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全自动放射性合成[18F]氟-C-糖基-c（RGDfC）：利用AllInOne合成器的所有功能

放射性标记的肽是用于生物医学研究目的的关键工具。肽通常通过间接修复基团方法用氟18标记，这需要一个不易自动化的复杂多步骤程序。但是，自动化是生产具有高可靠性和最少人员参与的放射性示踪剂的最重要的强制性步骤。此，我们描述[全自动化放射合成¹⁸ F]氟C ^上ALLINONE（AIO）合成-glyco-C（RDGfC），利用首次的AIO模块的所有能力。放射性示踪剂在高放射化学纯度制备通过140分钟内完成具有挑战性的三步操作序列，经衰变校正的放射化学产率为3.6±0.4％。呈现高的稳定性和改善的亲水性，[ ¹⁸ F]氟C ^ -glyco-C（RDGfC）可能会成为在PET成像中用于癌症诊断的重要工具。此外，所描述的自动化程序是模块化的，并且可以以最小的变化适用于其他假体基团和/或肽，以提供大量的¹⁸ F-放射性标记的肽。