Large-Scale Electrosynthesis of Borylated Azines

'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 thepharmaceutical sector.Azines are small-molecules integral to discover and manufacture pharmaceuticals andagrochemicals.

Using azines in Suzuki-Miyaura cross-coupling reactions represents the idealsolution to introduce these important motifs in discovery molecules but here is where theproblems 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, arehighly unstable.We urgently need chemical methods delivering borylated azines in a fast and cost-effectivemanner 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 photochemicalstrategies in radical chemistry, we recently identified a strategy that generates boryl radicalsand provides far greater capability over any other method to both prepare and utilizeborylated azines in modular fragment synthesis.B-ELECTRO aims to make the synthesis of our borylated azines workable on large scale andthus attractive to pharma and agro industries.This program provides a unique opportunity for the commercialization of our borylatedmaterials and their utilization by end-users, thus providing innovative chemistry solutions andlong-lasting impact to pharmaceutical and agrochemical industry and eventually our society.