Synthesis and In Vivo Imaging of a 18F‐Labeled PARP1 Inhibitor Using a Chemically Orthogonal Scavenger‐Assisted High‐Performance Method
- 21 January 2011
- journal article
- research article
- Published by Wiley in Angewandte Chemie International Edition in English
- Vol. 50 (8) , 1922-1925
- https://doi.org/10.1002/anie.201006579
Abstract
Pedal to the metal: The catalyst‐free Diels–Alder cycloaddition of trans‐cyclooctene and tetrazine was used to quickly and selectively generate an 18F‐labeled AZD2281 derivative from a tetrazine‐linked precursor. The probe was tested in biological assays, and its targeted accumulation was confirmed in vivo. This protocol allows the parallel synthesis of a library of potential PET imaging agents in a short time, thus increasing the efficiency of lead compound development.Keywords
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