Project description
Critical molecule for an essential process fosters pharmaceutical innovation
Azines are small molecules essential to pharmaceutical and agrochemical discovery and production. The palladium-catalysed coupling of a borylated molecule with an aryl halide (Suzuki-Miyaura cross-coupling) is one of the most important reactions in the pharmaceutical sector. Using borylated azines in Suzuki-Miyaura cross-coupling could foster innovation effectively, yet the borylation of azines is challenging, and when produced, borylated azines are highly unstable. The ERC-funded B_ELECTRO project plans to overcome these obstacles. The team has a new approach to generate boryl radicals that is vastly superior to other methods in enabling the preparation and utilisation of borylated azines in modular fragment synthesis. B_ELECTRO will support the team in upscaling their electrosynthesis of borylated azines.
Objective
                                'The Nobel prize-winning Suzuki-Miyaura cross-coupling involves the palladium-catalysed
coupling of a borylated molecule with an aryl halide and is the 2nd most used process by the
pharmaceutical sector.
Azines are small-molecules integral to discover and manufacture pharmaceuticals and
agrochemicals. Using azines in Suzuki-Miyaura cross-coupling reactions represents the ideal
solution to introduce these important motifs in discovery molecules but here is where the
problems come:
1. There is currently very limited way of borylating azines.
2. Borylated azines, especially the ones containing a boron vicinal to the N-atom, are
highly unstable.
We urgently need chemical methods delivering borylated azines in a fast and cost-effective
manner and that can then be employed in Suzuki-Miyaura cross-coupling reactions.
As part of our ERC-2018-StG NEBULAR, focused on the development of novel photochemical
strategies in radical chemistry, we recently identified a strategy that generates boryl radicals
and provides far greater capability over any other method to both prepare and utilize
borylated azines in modular fragment synthesis.
B-ELECTRO aims to make the synthesis of our borylated azines workable on large scale and
thus attractive to pharma and agro industries.
This program provides a unique opportunity for the commercialization of our borylated
materials and their utilization by end-users, thus providing innovative chemistry solutions and
long-lasting impact to pharmaceutical and agrochemical industry and eventually our society.
                            
            Programme(s)
            
              
              
                Multi-annual funding programmes that define the EU’s priorities for research and innovation.
                
              
            
          
                      Multi-annual funding programmes that define the EU’s priorities for research and innovation.
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                  HORIZON.1.1 - European Research Council (ERC)
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                  Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
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HORIZON-ERC-POC - HORIZON ERC Proof of Concept Grants
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              Call for proposal
                
                  
                  
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(opens in new window) ERC-2023-POC
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Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.
52062 Aachen
Germany
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