Tony Gee

DEVELOPMENT AND EVALUATION OF A NOVEL POSITRON EMISSION TOMOGRAPHY RADIOTRACER FOR IMAGING THE RECEPTOR FOR ADVANCED GLYCATION ENDPRODUCTS IN ALZHEIMER’S DISEASE: 2017 Abstract Supplement

Figure 1. Images from brain autoradiography experiments with sagittal brain sections of 8-month-old wild-type and 17-month-old transgenic (Tg2576) Alzheimer’s disease mice in the presence of 5 nM of [C]FPSZM1 (75 mM of FPS-ZM1 for non-specific binding (NSB)). Note the high level of NSB in either cerebellar or extracerebellar regions of the brain in each species. Specific binding is obtained by subtracting NSB from total binding (TB). Greater binding is denoted by red colour. Vilius Savickas, Salvatore Bongarzone, Federico Luzi, Nisha Singh, Tony D. Gee, National Institute for Health Research Biomedical Research Centre andGuy’s and St Thomas’ NHS Foundation Trust and King’s College London, London, United Kingdom; King’s College London, London, United Kingdom; King’s College London, London, United Kingdom. Contact e-mail: vilius.savickas@kcl.ac.uk

From [(11)C]CO2 to [(11)C]amides

Radiosynthesis of [11C]amides via the Mitsunobu reaction.

ESTABLISHMENT OF A PET RADIOTRACER NETWORK FOR DEMENTIA RESEARCH

differences in ADAS-cog sub-scores between the typical (Figure 1A) and parietal (Figure ID) subgroups estimated by SuStaln (p<0.05 shaded in blue). Parietal 1⁄4 AD patients with a higher probability of belonging to the parietal subtype (Figure 1D) than any of the other subtypes; Typical 1⁄4 AD patients with a higher probability of belonging to the typical subtype (Figure 1A) than any of the other subtypes; Strong Parietal 1⁄4 AD patients with probability>0.75 of belonging to the parietal subtype (Figure 1D); Strong Typical 1⁄4 AD patients with probability>0.75 of belonging to the typical subtype (Figure 1A). Poster Presentations: Saturday, July 15, 2017 P117

[ 11 C]CO 2 to [ 11 C]CO conversion mediated by [ 11 C]silanes

A novel chemical methodology is described for the conversion of [(11)C]CO2 to [(11)C]CO. Diphenylmethyl silanes trap [(11)C]CO2 and release [(11)C]CO rapidly when triggered by TBAF. Released [(11)C]CO was used to produce [(11)C]N-benzylbenzamide and AMPA receptor ligand, [(11)C], in radiochemical yields >90% within 6 min from [(11)C]CO2 production.

Transition metal mediated [C-11] carbonylation reactions

[(11) C]Carbon monoxide is undoubtedly a highly versatile radiolabelling synthon with many potential applications for the synthesis of positron emission tomography (PET) tracer molecules and functional groups, but why has it not found more applications in the PET radiolabelling arena? Today, (11) CO radiolabelling is still primarily viewed as a niche area; however, there are signs that this is beginning to change as some of the technical and chemistry challenges of producing, handling and reacting (11) CO are overcome. This mini review covers the more recent developments of (11) CO-labelling chemistry and is focused on palladium and rhodium-mediated carbonylation reactions that are growing in importance and finding wider application for carbon-11 PET radiotracer development.