Synthesis and in vivo imaging of a 18F-labeled PARP1 inhibitor using a chemically orthogonal scavenger-assisted high-performance method
Poly(ADP-ribose) Polymerase Inhibitors
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. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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