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• W1998644977 abstract "A new 18F-based prosthetic group has been prepared for the labeling of azide-modified peptides for use in PET imaging. 2-[18F]fluoro-3-(hex-5-ynyloxy)pyridine ([18F]FPy5yne, [18F]-1) was prepared via efficient nucleophilic heteroaromatic substitution of either the corresponding 2-nitro (2) or 2-trimethylammonium trifluoromethanesulfonate pyridine (3). Best radiochemical yield of [18F]FPy5yne from 2 was 91% by radioTLC (15 min, 110°C, DMSO). From 3, best radiochemical yield by radioTLC was 93% (15 min, 110°C, MeCN). HPLC-purified [18F]FPy5yne was ligated to model peptide N3–(CH2)4–CO–YKRI–OH by way of CuI-mediated Huisgen [3+2] cycloaddition in the presence of copper-stabilizing ligand tris(benzyltriazolylmethyl)amine (TBTA) and N,N-diisopropylethylamine (DIEA). Bioconjugate radiochemical yields were obtained in average yields of 89%±8.6% (n=4), as judged by radioHPLC. Best non-decay-corrected, collected radiochemical yield of modified peptide from end-of-bombardment was 5.8% (18.7% decay-corrected), with a total preparation time of 160 min from start of synthesis. Copyright © 2008 John Wiley & Sons, Ltd." @default.
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• W1998644977 date "2008-11-01" @default.
• W1998644977 modified "2023-09-27" @default.
• W1998644977 title "Radiosynthesis and bioconjugation of [¹⁸F]FPy5yne, a prosthetic group for the¹⁸F labeling of bioactive peptides" @default.
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• W1998644977 doi "https://doi.org/10.1002/jlcr.1561" @default.
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