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

Descripción del proyecto

Catálisis quiral avanzada

Las moléculas quirales pueden presentar dos formas especulares no superponibles, y su estructura correcta es esencial en productos farmacéuticos, fragancias y agroquímicos. Para producirlos de forma eficiente, los químicos emplean catalizadores y ligandos quirales que facilitan las transformaciones químicas clave. Sin embargo, la diversidad estructural de los ligandos disponibles es limitada, lo cual acota sus aplicaciones, y su producción suele lenta y cara. Para hacer frente a esta limitación, el proyecto AziPhos, financiado por el Consejo Europeo de Investigación, capitalizará el descubrimiento de una nueva clase de ligandos de fosfina quirales, los cuales se pueden sintetizar en un par de pasos a través de un proceso catalítico eficiente. Se prevé que este planteamiento mejore de forma notable la síntesis asimétrica y posibilite el desarrollo de nuevos fármacos quirales.

Objetivo

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.