The expansion of [<sup>18</sup>F]-radiolabelling methodologies is vital for the advancement of Positron Emission Tomography (PET) as a medical imaging tool. Novel protocols will simplify access to current PET tracers and allow development of original tracers, potentially enhancing the imaging quality or permit imaging of a wider range of clinical problems. A general introduction is presented in <b>Chapter 1</b>, covering PET, application of fluorine-19 in the pharmaceutical industry, the production of fluorine-18 and the current state-of -art for [<sup>18</sup>F]-radiolabelling. The results chapters are divided in to two parts; <b>Part 1</b> (<b>Chapters 2 - 4</b>) concern the synthesis of [18F]fluoroarenes and <b>Part II</b> (<b>Chapters 5</b> and <b>6</b>) discuss diversity oriented radiofluorination techniques, targeting novel [<sup>18</sup>F]motifs. In <b>Part I</b>, Chapter 2 describes the use of hypervalent iodine reagents to meditate an umpolung approach for fluorination and radiofluorination of N-arylsulfonamides and anilides. <b>Chapter 3</b> again utilises hypervalent iodine reagents, but as spirocyclic iodonium(III) ylide precursors, being applied to semi-automated and automated microfluidic conditions. <b>Chapter 4</b> discusses the development of conditions for the production and isolation of radiopharmaceuticals employing Cu(II)-mediated radiofluorination of aryl boronic pinacol esters. In <b>Part II, Chapter 5</b> discusses the applicability of halogen exchange reactions to reach polyfluorinated motfis and <b>Chapter 6</b> focuses on the application of a single diazo precursor to access three polyfluorinated motifs with single-step reactions. Finally, <b>Chapter 7</b> provides experimental data for compounds discussed in this thesis.
| Identifer | oai:union.ndltd.org:bl.uk/oai:ethos.bl.uk:730136 |
| Date | January 2016 |
| Creators | Calderwood, Samuel |
| Contributors | Gouverneur, Véronique |
| Publisher | University of Oxford |
| Source Sets | Ethos UK |
| Detected Language | English |
| Type | Electronic Thesis or Dissertation |
| Source | https://ora.ox.ac.uk/objects/uuid:9cd31311-0825-4f10-bd84-8568191175f7 |
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