title: New strategy for the preparation of clickable peptides and labeling with 1-(azidomethyl)-4-[(18)F]-fluorobenzene for PET.
abstract: 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-[(18)F]-fluorobenzene) has been produced in a four step procedure in 75 min with a 34% radiochemical yield (decay corrected). Conjugation of [(18)F]fluoroazide with a model alkyne-neuropeptide produced the desired (18)F-radiolabeled peptide in less than 15 min with a yield of 90% and excellent radiochemical purity.
authors.affiliation: Cyclotron Research Center, Liege University, Belgium. dthonon@ulg.ac.be
authors.forename: David
authors.initials: D
authors.lastname: Thonon
authors.forename: Cécile
authors.initials: C
authors.lastname: Kech
authors.forename: Jérôme
authors.initials: J
authors.lastname: Paris
authors.forename: Christian
authors.initials: C
authors.lastname: Lemaire
authors.forename: André
authors.initials: A
authors.lastname: Luxen