A One-Pot Radio-synthesis of [18F]PARPi

In this paper, we disclose a new strategy for the radio-synthesis of [ 18 F]PARPi from the corresponding, boc-protected, nitro-precursor. Using a two-step procedure, [ 18 F]PARPi could be isolated in radiochemical yields up to 9.6%. The reaction proceeds via an efficient one-pot, two-step process, allowing for simplification over previous methods that require complex multi-step, multi-pot strategies to be implemented. In this work, we present a novel radio-synthesis of 18 F-PARPi, an imaging agent for PARP1 expression. 18 F-PARPi was synthesized by nucleophilic aromatic substitution of the corresponding boc-protected nitro-precursor followed by acidic deprotection.