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Lack of radiochemical methods to introduce radioactive labels into small molecules and large macromolecules alike limits the pharmacological space that is accessible with nuclear imaging.
We develop new chemical platform techniques that give access to an unprecedented radiochemical space and allow flexible radiotracer design and manufacture in clinical routine.
Sulfonium salt chemistry for aromatic labelling with fluorine-18
Sulfonium salts allow direct labelling of small drug-like molecules with fluorine-18. The appeal of this approach is the ability to label a broad range of bioactive molecules under conditions that mirror conventional substitution reactions with fluoride-18. With the aim to overcome the synthetic limitations associated with sulfonium salt formation, we developed a novel intramolecular ring-closing reaction that gives access to highly functionalized dibenzothiophene sulfonium salts. The strategy provides a flexible platform, and facilitates the development of novel radiotracers for imaging with positron emission tomography.
References: Sander, Sci Rep 2015 | Gendron, JACS 2018
Iodine click chemistry for multimodality imaging probes
The ability to study biological processes across the cellular and macroscopic scales remains a fundamental goal for molecular imaging. However, no imaging modality meets the need for high resolution, high sensitivity, and deep tissue penetration. With the aim to address this need we developed a new approach to multiscale multimodal imaging based on a one‐pot synthesis of dual optical and nuclear labelling reagents, and applied it to dual labelling of an antibody.
References: Yan, Angew Chem 2011 | Yan, JACS 2013