Synthesis and In Vivo Imaging of a 18F‐Labeled PARP1 Inhibitor Using a Chemically Orthogonal Scavenger‐Assisted High‐Performance Method

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.