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Synthesis of Radiotracers to Image Neuroinflammation in Alzheimer’s Disease

Year: 2025
Type: conference-paper
Abstract: Alzheimer’s disease (AD) remains one of the most devastating neurodegenerative disorders, with 10 million new cases reported every year. Despite decades of research, its early and accurate diagnosis continues to pose a major clinical challenge, emphasizing the need for sensitive molecular imaging techniques. Positron emission tomography (PET) imaging, through the use of specific radiotracers, offers a powerful tool to visualize and quantify key molecular targets involved in the disease [1]. Among these targets, Monoamine Oxidase-B (MAO-B) has emerged as a promising biomarker for early AD detection, as it is massively upregulated during the neuroinflammatory phase occurring in the early stages of the disease [2]. [¹⁸F]SMBT-1, a well-established radiotracer for MAO-B [3], has proven to be a highly promising candidate, although its synthesis has so far remained difficult to achieve reliably. The overarching aim of this project is therefore to develop a robust, reliable, and straightforward automated radiosynthesis process suitable for routine clinical production of [¹⁸F]SMBT-1. Our first objective was to synthesize the non-radioactive SMBT-1, which served (i) to investigate protection and deprotection strategies and (ii) as an analytical reference for the development of QC methods and confirmation of the radiotracer’s identity. In a second step, the synthesis of the tosylated precursor was undertaken to enable the subsequent incorporation of radioactive fluorine-18. Initial radiolabelling experiments proved challenging, with radiochemical yields below 5%. Further investigation identified contamination with trace amounts of chloride and chlorinated analogues as a potential cause. To address this, alternative synthetic routes were explored, focusing on the reactivity of tosylated epoxides, allyl derivatives, and the various alcohol groups within the molecule.
Language: English
Field: Medicine
Open Access status: green
OpenAlex ID: W7123381919
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