New Strategy for the Preparation of Clickable Peptides and Labeling with 1-(Azidomethyl)-4-[18F]-fluorobenzene for PET

[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

Volume :

Issue :

Pages :

817-823

Peer reviewed :

Peer Reviewed verified by ORBi

Available on ORBi :

since 05 August 2010

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