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Title: Radiolabelling of aryl boronic esters with 18F and 123I : method development and application
Author: McSweeney, Greg
ISNI:       0000 0004 7652 1662
Awarding Body: University of Oxford
Current Institution: University of Oxford
Date of Award: 2017
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The overarching theme of this thesis is the application of aryl boronic esters to the fields of PET and SPECT radiochemistry. Chapter 1 provides an introduction to positron emission tomography (PET) and single photon emission computed tomography (SPECT), in conjunction with an introduction to the utility of arylboranes as precursors for radioisotope incorporation. In chapter 2, a general method for the copper-mediated nucleophilic 123I-iodination of (hetero)aryl boronic pinacol esters and acids is disclosed. This methodology was applied toward the successful radiosynthesis of four commonly used SPECT radiotracers, [123I]DPA- 713, [123I]IMPY, [123I]MIBG and [123I]IPEB. In chapter 3, the copper-mediated nucleophilic 18F-fluorination of aryl boronic pinacol esters, developed in the Gouverneur group, has been applied to the field of prosthetic group 18F-radiochemistry. This protocol was utilised to synthesise four popular prosthetic groups in a single radiosynthetic step. Chapter 4 describes the radiosynthesis and biological evaluation of [18F]DPA-713 and [18F]CF3DPA-713, two novel analogues of the Translocator Protein (TSPO) ligand N,N-diethyl-2-(4-methoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3- acetamide-713 (DPA-713). Finally, chapter 5 details experimental procedures and characterisation for all compounds.
Supervisor: Gouverneur, Veronique Sponsor: Engineering and Physical Sciences Research Council
Qualification Name: Thesis (Ph.D.) Qualification Level: Doctoral
EThOS ID:  DOI: Not available