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Large-Scale Electrosynthesis of Borylated Azines

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.

Fields of science (EuroSciVoc)

Programme(s)

Topic(s)

Funding Scheme

HORIZON-ERC-POC - HORIZON ERC Proof of Concept Grants

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Call for proposal

(opens in new window) ERC-2023-POC

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Host institution

RHEINISCH-WESTFAELISCHE TECHNISCHE HOCHSCHULE AACHEN
Net EU contribution
€ 150 000,00
Address
TEMPLERGRABEN 55
52062 Aachen
Germany
Region
Nordrhein-Westfalen Köln Städteregion Aachen
Activity type
Higher or Secondary Education Establishments
Links
Total cost
No data

Beneficiaries (1)