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

Introduction

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.

Current Challenges

Despite these advances, the number of chemical transformations required to produce chiral molecules continues to grow. However, 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.

Limitations of Existing Ligands

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.

Proposal Overview

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.

Advantages of New Ligands

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.