Large-Scale Electrosynthesis of Borylated Azines

'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.