Abstract
Positron emission tomography (PET) is a non-invasive molecular imaging technique that provides quantitative and qualitative data on the biodistribution of radiolabelled molecules in vivo. Among the positron (β+) emitting radionuclides used in PET radiopharmaceutical production, carbon-11 (11C, radioactive half-life = 20.4 min) is a valuable choice due to the ubiquity of carbon atoms into biologically-active organic molecules and the preservation of biological characteristics upon isotopic substitution of carbon-12. Cyclotron products of 11C is usually obtained as [11C]CO2, which presents limited reactivity and often requires conversion into more reactive labelling agents (e.g. [11C]CH3I) via time-consuming processes that contrast with the short half-life of 11C. The development of novel strategies to enhance the reactivity of [11C]CO2 would avoid the need of synthon conversion steps and would shorten the total processing time for radiopharmaceutical production.This thesis discusses the development of a novel methodology for 11C-formylation from [11C]CO2. In spite of the wide chemical reactivity and presence in biologically-active molecules, the 11C-labelling on the formyl group has not yet been developed, limiting the access to this important class of compounds.
The thesis will also discuss the development of a novel methodology for 11C-methoxylation from [11C]CO2. This methodology utilises organosilyl reagents and compared to current O-11C-methylation procedures with [11C]CH3I does not require time-consuming synthon conversion steps or synthon-dedicated synthesis units.
The application of these methodologies will expand the pool of molecules available for radiolabelling and the number of applications in PET imaging.
Date of Award | 1 Jun 2022 |
---|---|
Original language | English |
Awarding Institution |
|
Supervisor | Tony Gee (Supervisor), Salvatore Bongarzone (Supervisor) & Philip Blower (Supervisor) |