A Leap in Ligand Technology: The Development and Valorization of Novel Chiral Diphosphine Ligands

Description du projet

Une catalyse chirale avancée

Les molécules chirales existent sous deux formes inversées, et leur structure correcte est essentielle pour les produits pharmaceutiques, les parfums et les produits agrochimiques. Pour les produire efficacement, les chimistes utilisent des catalyseurs et des ligands chiraux qui favorisent des transformations chimiques importantes. Cependant, la diversité structurelle des ligands disponibles est limitée, ce qui restreint leurs applications, et leur production s’avère souvent coûteuse et longue. Pour y remédier, le projet AziPhos, financé par le CER, s’appuie sur la découverte révolutionnaire d’une nouvelle classe de ligands phosphines chiraux qui peuvent être synthétisés en quelques étapes seulement grâce à un processus catalytique robuste. Cette approche devrait faire considérablement progresser la synthèse asymétrique et ouvrir la voie à de nouveaux médicaments chiraux.

Objectif

The search for innovative and efficient chiral catalysts and ligands for producing enantiopure molecules remains a vital priority across the pharmaceutical, flavours and fragrances, and agrochemical sectors. A significant majority of newly developed drugs are chiral, creating an increasing demand for advancements in asymmetric synthesis and the development of chiral ligands and metal complexes, which is driving substantial progress in asymmetric catalysis. Despite these advances, the number of chemical transformations required to produce chiral molecules continues to grow, while only a small fraction of the hundreds of chiral ligands developed for use in chiral catalysts have been commercialized, and even fewer have been successfully scaled for industrial applications.
The most successful ligands, often referred to as ‘privileged phosphine ligands,’ have achieved notable success in various transformations. However, their structural diversity is limited, constraining further expansion of reactivity, and their production costs remain high. Most of these successful chiral phosphine ligands require multi-step, time-consuming, and costly non-catalytic synthetic routes.
In this context, this proposal aims to build upon a recent breakthrough—the discovery of a completely new class of highly efficient chiral phosphine ligands. Notably, these ligands offer a significant advantage by being producible via a robust catalytic synthesis that requires only 1-2 steps. Moreover, the structure of this new ligand family is highly modular, allowing for rapid diversification and the creation of a library of related ligands.
These promising features suggest that our discovery holds the potential to develop a product with a compelling value proposition, representing a significant advancement over current competing solutions in the market.