Click for PET:: rapid preparation of [18F]fluoropeptides using CuI catalyzed 1,3-dipolar cycloaddition

Cu-I catalyzed 1,3-dipolar cycloaddition 'click chemistry' was used to prepare F-18-radiolabeled peptides. Three omega-[F-18]-fluoroalkynes were prepared in yields 1 ranging from 36% to 81%. Conjugation of omega-[F-18]fluoroalkynes to various peptides decorated with 3-azidopropionic acid via Cu-I mediated 1,3-dipolar cycloaddition yielded the desired F-18-labeled products in 10 min with yields of 54-99% and excellent radiochemical purity (81-99%). The total synthesis time was 30 min from the end of bombardment. (c) 2006 Elsevier Ltd. All rights reserved.