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Title: Synthesis of [18F]RGD-K5 by catalyzed [3 + 2] cycloaddition for imaging integrin αvβ3 expression in vivo
Authors: Mirfeizi, Leila ×
Walsh, Joe
Kolb, Hartmuth
Campbell-Verduyn, Lachlan
Dierckx, Rudi A
Feringa, Ben L
Elsinga, Philip H
de Groot, Tjibbe
Sannen, Ivan
Bormans, Guy
Celen, Sofie #
Issue Date: Jul-2013
Publisher: Pergamon Press
Series Title: Nuclear Medicine and Biology vol:40 issue:5 pages:710-6
Article number: 10.1016/j.nucmedbio.2013.04.003
Abstract: In the last few years click chemistry reactions, and in particular copper-catalyzed cycloadditions have been used extensively for the preparation of new bioconjugated molecules such as (18)F-radiolabeled radiopharmaceuticals for positron emission tomography (PET). This study is focused on the synthesis of the Siemens imaging biomarker [(18)F]RGD-K5. This cyclic peptide contains an amino acid sequence which is a well known binding motif for integrin αvβ3 involved in cellular adhesion to the extracellular matrix. We developed an improved "click" chemistry method using Cu(I)-Monophos as catalyst to conjugate [(18)F]fluoropentyne to the RGD-azide precursor yielding [(18)F]RGD-K5. A comparison is made with the registered Siemens method with respect to synthesis, purification and quality control. [(18)F]RGD-K5 was obtained after 75 min overall synthesis time with an overall radiochemical yield of 35% (EOB). The radiochemical purity was >98% and the specific radioactivity was 100-200 GBq/μmol at the EOS.
URI: 
ISSN: 0969-8051
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Radiopharmacy
× corresponding author
# (joint) last author

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