Automated preparation of 2‐[18F]fluoropropionate labeled peptides using a flexible,multi‐stage synthesis platform (iPHASE Flexlab) |
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Authors: | Mohammad B Haskali Peter D Roselt Rodney J Hicks Craig A Hutton |
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Institution: | 1. School of Chemistry, The University of Melbourne, Melbourne, Victoria, Australia;2. Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, Victoria, Australia;3. The Centre for Molecular Imaging and Translational Research Laboratory, The Peter MacCallum Cancer Centre, Melbourne, Victoria, Australia |
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Abstract: | Radiolabelled peptides are vital tools used in positron emission tomography imaging for the diagnosis of disease, drug discovery, and biomedical research. Peptides are typically labeled through conjugation to a radiolabelled prosthetic group, which usually necessitates complex, multi‐step procedures, especially for fluorine‐18 labeled peptides. Herein, we describe the automated synthesis and formulation of 2‐18F]fluoropropionate labeled RGD‐peptides through use of the iPHASE Flexlab as an effective dual‐stage radiochemical synthesis module. The fully automated preparation of the monomeric RGD‐peptides, 18F]FP‐GalactoRGD and 18F]FP‐c(RGDy(SO3)K), was accomplished in under 90 minutes with n.d.c. radiochemical yields ca. 7% from fluoride. Similarly, the automated preparation of the dimeric RGD‐peptides, 18F]F‐PRGD2 and 18F]FP‐E(RGDy(SO3)K)2, was accomplished in under 105 minutes with n.d.c. yields ca. 4% from fluoride. |
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Keywords: | automation F‐18 PET PET chemistry radiosynthesis |
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