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Site‐Selective,Late‐Stage C−H 18F‐Fluorination on Unprotected Peptides for Positron Emission Tomography Imaging |
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| Authors: | Dr. Zheliang Yuan Dr. Matthew B. Nodwell Dr. Hua Yang Dr. Noeen Malik Helen Merkens Dr. François Bénard Dr. Rainer E. Martin Dr. Paul Schaffer Prof. Robert Britton |
| Affiliation: | 1. Department of Chemistry, Simon Fraser University Burnaby, British Columbia, Canada;2. Life Science Division, TRIUMF, Vancouver, BC, Canada;3. Department of Molecular Oncology, BC Cancer Agency, Vancouver, British Columbia, Canada;4. Medicinal Chemistry, Roche Pharma Research and Early Development (pRED), Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd, Basel, Switzerland |
| Abstract: | Peptides are often ideal ligands for diagnostic molecular imaging due to their ease of synthesis and tuneable targeting properties. However, labelling unmodified peptides with 18F for positron emission tomography (PET) imaging presents a number of challenges. Here we show the combination of photoactivated sodium decatungstate and [18F]‐N‐fluorobenzenesulfonimide effects site‐selective 18F‐fluorination at the branched position in leucine residues in unprotected and unaltered peptides. This streamlined process provides a means to directly convert native peptides into PET imaging agents under mild aqueous conditions, enabling rapid discovery and development of peptide‐based molecular imaging tools. |
| Keywords: | 18F-fluorination photocatalysis peptides PET imaging radiolabeling |