An improved radiosynthesis of O-(2-[¹⁸ F]fluoroethyl)-O-(p-nitrophenyl)methylphosphonate: A first-in-class cholinesterase PET tracer.

ABSTRACT: O-(2-Fluoroethyl)-O-(p-nitrophenyl) methylphosphonate 1 is an organophosphate cholinesterase inhibitor that creates a phosphonyl-serine covalent adduct at the enzyme active site blocking cholinesterase activity in vivo. The corresponding radiolabeled O-(2-[¹⁸ F]fluoroethyl)-O-(p-nitrophenyl) methylphosphonate, [¹⁸ F]1, has been previously prepared and found to be an excellent positron emission tomography imaging tracer for assessment of cholinesterases in live brain, peripheral tissues, and blood. However, the previously reported [¹⁸ F]1 tracer synthesis was slow even with microwave acceleration, required high-performance liquid chromatography separation of the tracer from impurities, and gave less optimal radiochemical yields. In this paper, we report a ne

SUBMITTER: Neumann KD 

PROVIDER: S-EPMC6031433 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature