Radiosynthesis and bioconjugation of [18F] FPy5yne, a prosthetic group for the 18F labeling of bioactive peptides

JAH Inkster, B Guérin, TJ Ruth…

Index: Inkster, James A. H.; Guerin, Brigitte; Ruth, Thomas J.; Adam, Michael J. Journal of Labelled Compounds and Radiopharmaceuticals, 2008 , vol. 51, # 14 p. 444 - 452

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Citation Number: 39

Abstract

Abstract A new 18 F-based prosthetic group has been prepared for the labeling of azide- modified peptides for use in PET imaging. 2-[18 F] fluoro-3-(hex-5-ynyloxy) pyridine ([18 F] FPy5yne,[18 F]-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 [18 F] FPy5yne from 2 was 91% by radioTLC (15 ...