High‐Yielding, Two‐Step ¹⁸F Labeling Strategy for ¹⁸F‐PARP1 Inhibitors

Speedy and easy! An 18F-labeled PARP1 imaging agent, based on AZD2281, was prepared via an inverse electron demand Diels–Alder cycloaddition in high radiochemical yield for positron emission tomography (PET) imaging. This strain-promoted ‘bioorthogonal’ reaction is envisioned to be a widely applicable 18F-labeling strategy for repeat and on-demand synthesis of small molecules for PET imaging.