Project description
Fast synthesis of labelled organic compounds for drug development and food safety studies
Radioactive labelling is a process frequently used before products reach the market in drug research and development, food research and agricultural chemistry. This process allows researchers to track the movement or breakdown of target molecules by following their radioactivity. Carbon-14 is a naturally occurring isotope but its use in the labelling of molecules presents many disadvantages, including the production of radioactive waste, multi-step time-consuming processes and high use of resources. The EU-funded FASTLabEx project plans to demonstrate a novel approach for the straightforward preparation of carbon-labelled complex organic molecules that overcomes fundamental limitations. The radioactive tag will be introduced at the ultimate stage of the organic molecule synthesis. A simpler, faster and more efficient access to carbon labelled molecules will help supporting drug development and ensure safety and appropriate administration of medicine to patients.
Objective
The impact of synthetic organic molecules on health, life quality and lifestyle is beyond doubt. It is therefore of fundamental importance to detect and quantify the fate of organic compounds and provide a precise risk/benefit assessment, before they reach the market and large public exposure. The traceless incorporation of carbon-14 allows tracking organic molecules and provides vital knowledge on their fate. This information is critical for pharmaceutical development, crop science and human food safety evaluation. Surprisingly, carbon radiolabeling still represents a bottleneck and an unsolved fundamental problem. In fact, current synthetic strategies are marred by several major drawbacks, including the generation of radioactive waste, being multi-step time-consuming and high resource-demanding. To circumvent such disadvantages, I present FASTLabEx, a novel approach for the straightforward preparation of carbon-labeled complex organic molecules that introduces the radioactive tag at the ultimate-stage of the synthesis. Inspired by efficient metal-catalyzed transformations, FASTLabEx makes use of a novel paradigm of “carbon isotope exchange”, defined as the selective replacement of molecular moieties into organic molecules, by reversible molecular deconstruction/reconstruction in presence of an appropriate radiolabeled moiety. FASTLabEx will explore this concept onto a large variety of functional groups and structural diversity, far beyond the case of carboxylic acids. This approach has the potential to streamline the radio-synthesis of pharmaceuticals and agrochemicals. Outcomes from FASTLabEx will have a tangible societal impact not only for the radiochemical community, but also for pharmaceutical and agrochemical industries and in fine the consumers and patients. In order to mitigate the risks inherent to the project, preliminary results demonstrate its feasibility.
Fields of science
- engineering and technologyother engineering and technologiesnuclear engineeringnuclear waste management
- natural scienceschemical sciencesorganic chemistryorganic acids
- medical and health sciencesbasic medicinepharmacology and pharmacypharmaceutical drugs
- engineering and technologyother engineering and technologiesfood technologyfood safety
- agricultural sciencesagriculture, forestry, and fisheriesagriculture
Programme(s)
Funding Scheme
ERC-COG - Consolidator GrantHost institution
75015 PARIS 15
France