SELEFLU

Synthesis and Evaluation of 18F-Labelled N-F Reagents

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 Obiettivo del progetto (Objective)

'The overall objective of this proposal is to capitalise on our expertise in synthetic and fluorine organic chemistry by undertaking a research programme aimed at exploring the value of 18F-labelled N-F reagents. Upon completion of the proposed research programme, we hope to provide 18F-radiochemists with a toolbox filled with novel 18F-radiosynthetic strategies. The unconventional and innovative methods that we will investigate are designed to address well recognised pending problems in 18F-radiolabelling and to offer unprecedented radiosynthetic routes to access 18F-labelled targets. The impact of the novel radiochemistry we propose to develop is far reaching to advance Positron Emission Tomography (PET). PET is a non-invasive molecular imaging technique used clinically for diagnostic purpose and drug discovery. This expanding highly interdisciplinary area of research relies on radiotracers labelled with a positron-emitting radioisotope. 18F-Labelled molecules are frequently used because of the advantageous properties of the 18F in comparison with other non-metallic radioisotopes. For rapid progress, the radiochemistry available for 18F-labelling should be sufficiently diverse for any designed 18F-radiotracers to be accessible regardless of the point of attachment of the 18F-label. To date, this is far from the reality, as current methodologies to construct 18F-labelled molecules present with limitations. The emphasis of this proposal is on the development and use of 18F-labelled N-F reagents of high specific activity for electrophilic fluorination. These reagents should allow for the production of 18F-labelled radiotracers in high radiochemical yield, purity and specific activity.'

Introduzione (Teaser)

Clinical applications of positron emission tomography (PET) have increased thanks to the widespread distribution of one molecule, fluorine-18. A synthesis toolbox developed by EU-funded scientists will produce new fluorine-18 radiotracers for even more efficient and reliable PET.

Descrizione progetto (Article)

Over the past decade, PET has become a powerful clinical imaging tool for evaluating complex biochemical processes in cancer patients. Measurements of "normal" and altered biochemical pathways are routinely performed. But the continued growth of PET requires the expansion of available positron-emitting radiopharmaceuticals.

Given that fluorine-18 can act as a radiotracer in PET, it was no surprise that chemists working on the 'Synthesis and evaluation of 18F-labelled N-F reagents' (SELEFLU) project have given special attention to this radioactive isotope. Fluorine-18 is the 13th most abundant element in the Earth's crust; and yet only 21 biosynthesised natural molecules containing fluorine are known.

The SELEFLU chemists developed and evaluated new methods to incorporate fluorine into organic molecules by making carbon-fluorine bonds. The new bond-forming reactions allow access to organic molecules of PET tracers under copper catalysis. The so-called trifluoromethylation could be performed using iodine reagents, combining a benign environmental character with commercial availability.

In addition to copper-mediated catalysis, the SELEFLU scientists have succeeded in harnessing the energy of visible light for the trifluoromethylation of silicon-containing molecules. Furthermore, new methods for labelling aromatic hydrocarbons with fluorine-18 were developed and validated. These methods should increase the number of radiopharmaceuticals routinely used in PET.

SELEFLU approaches to the introduction of fluorine-18 into organic molecules have introduced a fluorine-18 chemistry characterised by high selectivity and unique efficiency. Hopefully, complicated work-up procedures will become obsolete. And the improvements in synthesis of radiopharmaceuticals should offer new possibilities for the development of drugs, especially for central nervous system diseases.