No carrier-added nucleophilic aromatic radiofluorination using solid phase supported arenediazonium sulfonates and 1-(aryldiazenyl)piperazines

Abstract This Letter concerns the investigation of a solid phase based method for no carrier-added nucleophilic [ 18 F]fluorination of aromatic compounds via de-diazofluorination. Initial screening of reaction conditions was conducted using soluble analogues, that is, substituted benzenediazonium tosylates and 1-(phenyldiazenyl)piperazines in solution. This was followed by translation of the principle conditions to solid phase bound analogues. A variety of substituted aryldiazonium cations were immobilised using a sulfonate functionalised ion exchange resin and labelled with [ 18 F]fluoride ion by Balz–Schiemann like thermal decomposition in the presence of no carrier-added [ 18 F]fluoride …

Characterisation of [11C]PR04.MZ in Papio anubis baboon: A selective high-affinity radioligand for quantitative imaging of the dopamine transporter

N-(4-fluorobut-2-yn-1-yl)-2β-carbomethoxy-3β-(4′-tolyl)nortropane (PR04.MZ, 1) is a PET radioligand for the non-invasive exploration of the function of the cerebral dopamine transporter (DAT). A reliable automated process for routine production of the carbon-11 labelled analogue [11C]PR04.MZ ([11C]-1) has been developed using GMP compliant equipment. An adult female Papio anubis baboon was studied using a test–retest protocol with [11C]-1 in order to assess test–retest reliability, metabolism and CNS distribution profile of the tracer in non-human primates. Blood sampling was performed throughout the studies for determination of the free fraction in plasma (fP), plasma input functions and m…

Automated GMP production of [11C]PR04.MZ via the captive solvent method and PET studies in non-human primates: A promising tracer for extrastriatal DAT imaging