A one‐pot radiosynthesis of [¹⁸F]PARPi

Abstract

In this paper, we disclose a new strategy for the radiosynthesis of [18F]PARPi from the corresponding, boc‐protected, nitro‐precursor. Using a two‐step procedure, [18F]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.

Fully Automated, High-Dose Radiosynthesis of [18F]PARPi

“…RCY was 9.6%. Furthermore, the required precursor is, to our knowledge, not commercially available, and the highest starting activity used was 992 MBq [12].…”

Two experts and a newbie: [18F]PARPi vs [18F]FTT vs [18F]FPyPARP—a comparison of PARP imaging agents

“…While [ 18 F]FTT radiosynthesis only requires one step, [ 18 F]PARPi synthesis developed by Carney et al [ 22 ] involves many additions of low reagent volumes and has not been automated in literature. We instead successfully used our established automated [ 18 F]SFB labeling protocol for synthesis of this compound although during the preparation of the manuscript, a one-pot synthesis of [ 18 F]PARPi has been published by Wilson et al [ 37 ]. To synthesize the novel variant [ 18 F]FPyPARP, we designed a one-pot reaction utilizing the synthon [ 18 F]FPyTFP.…”

Advancements in PARP1 Targeted Nuclear Imaging and Theranostic Probes

“…Both tracers have similar structures: 18 F-PARPi and 18 F-20 have fluorobenzamide and methylfluorobenzamide moieties respectively in place of the isopropyl moiety of olaparib [15,16]. Recently, a simplified process for the synthesis of 18 F-PARPi has been reported, reducing the synthesis time from 90 min to 66 min, although the radiochemical yield obtained was 9.6% compared to 10% reported earlier [36]. Both 18 F-PARPi and 18 F-20 have been shown in subcutaneous models promising tumor-to-muscle ratios of 5.1 ± 0.9 and 3.6 ± 0.5, respectively.…”