Fully automated radiosynthesis of [F]fluoro--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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Published in | Reaction chemistry & engineering Vol. 4; no. 12; pp. 288 - 298 |
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Main Authors | , , , , , |
Format | Journal Article |
Language | English |
Published |
19.11.2019
|
Online Access | Get full text |
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Summary: | 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. |
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Bibliography: | 10.1039/c9re00303g Electronic supplementary information (ESI) available: Experimental section, HPLC chromatograms and AIO radioactivity trending. See DOI |
ISSN: | 2058-9883 |
DOI: | 10.1039/c9re00303g |