[en] The alkyne-azide Cu(I)-catalyzed Huisgen cycloaddition, a click type reaction was used to label a peptide with
fluorine-18. A novel solid phase synthesis approach for the preparation of clickable peptides has been developed
and has also permitted the straightforward preparation of reference compounds. A complementary azide labeling
agent (1-(azidomethyl)-4-[18F]-fluorobenzene) has been produced in a four step procedure in 75 min with a 34%
radiochemical yield (decay corrected). Conjugation of [18F]fluoroazide with a model alkyne-neuropeptide produced
the desired 18F-radiolabeled peptide in less than 15 min with a yield of 90% and excellent radiochemical purity
Disciplines :
Chemistry
Author, co-author :
Thonon, David ; Université de Liège - ULiège > Centre de recherches du cyclotron
Paris, Jérôme ; Université de Liège - ULiège > Centre de recherches du cyclotron
Kech, Cecile
Lemaire, Christian ; Université de Liège - ULiège > Centre de recherches du cyclotron
Luxen, André ; Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse - Centre de recherches du cyclotron
Language :
English
Title :
New Strategy for the Preparation of Clickable Peptides and Labeling with 1-(Azidomethyl)-4-[18F]-fluorobenzene for PET
Publication date :
26 March 2009
Journal title :
Bioconjugate Chemistry
ISSN :
1043-1802
eISSN :
1520-4812
Publisher :
American Chemical Society, Washington, United States - District of Columbia
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