Summary
'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.
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.
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More information & hyperlinks
| Web resources: | https://cordis.europa.eu/project/id/101123087 |
| Start date: | 01-01-2024 |
| End date: | 30-06-2025 |
| Total budget - Public funding: | - 150 000,00 Euro |
Cordis data
Original description
'The Nobel prize-winning Suzuki-Miyaura cross-coupling involves the palladium-catalysedcoupling 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.
Status
SIGNEDCall topic
ERC-2023-POCUpdate Date
12-03-2024
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