A one‐pot radiosynthesis of [18F]PARPi. (16th June 2020)

• Record Type: Journal Article
• Authors: Wilson, Thomas C.; Pillarsetty, Nagavarakishore; Reiner, Thomas
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 63:Number 9(2020)
• Page Start: 419
• Page End: 425
• Publication Date: 2020-06-16
• Subjects: [18F]PARPi -- fluorine‐18 -- Olaparib -- PARP inhibitor -- PET chemistry -- radiochemistry; Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3847
• Languages: English
• ISSNs: 0362-4803

Abstract

Abstract : In this paper, we disclose a new strategy for the radiosynthesis 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. Abstract : In this work, we present a novel radiosynthesis 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.