Project description
Going with the flow leads to novel molecular constructs for the pharmaceutical industry
Continuous flow processing in which solutions of reagents are pumped through tubes at known rates is emerging as an important alternative to traditional batch-reactor processes for pharmaceutical manufacturing. It can improve control of quality, reduce costs and time, and enhance sustainability. As a key enabling technology for the future of pharmaceutical manufacturing, it is also strongly supported by regulatory bodies. The EU-funded FI4P project is developing a protocol building on the benefits of flow chemistry and the use of iron as an abundant and benign catalyst. The process will enable access to reactions of relevance to the pharmaceutical industry incompatible with other processes. Controlled assembly of molecular scaffolds of therapeutic interest will pave the way to an enhanced library for fragment-based drug design.
Objective
The demand for sustainable methods to build chemical bonds has led to the rise of catalytic reactions, especially using abundant and benign metals. In this context, iron has emerged as a powerful catalyst to mediate various transformations including cross-couplings between (pseudo)halide electrophilic partners and organometallic nucleophiles, usually Grignard reagents.
We aim to develop a modular and versatile Flow-enabled Iron-catalysed cross-coupling protocol for Pharmaceutical applications (FI4P), leveraging the unique properties of flow chemistry to implement cross-couplings between organolithium derivatives and electrophiles. Building on the significant expertise of the academic host in this field, we will seek to harness flow technology to exert spatiotemporal control over reactive intermediates, thus ensuring the functionalisation of halide precursors with reactive lithium organyls generated in situ. The particularly high reaction rates observed in iron-catalysed cross-couplings will allow the incorporation of valuable functional groups usually incompatible with organolithium derivatives.
This approach will deliver a sustainable method to assemble relevant molecular scaffolds of interest to the pharmaceutical industry. With the involvement of NovAliX, an industrial partner specialised in transferring academic innovations into industrial processes, we will eventually apply our synthetic protocol to the large-scale manufacture of valuable APIs and the generation of a small collection of molecules designed to complement our existing library for Fragment Based Drug Design.
Fields of science
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CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques.
Programme(s)
Funding Scheme
MSCA-IF-EF-ST - Standard EFCoordinator
4000 Liege
Belgium