ILLUMINATING ROUTES TO 3D ORGANOBORON MOLECULES

Introduction

With a steadily growing, aging population, there is significant strain on the pharmaceutical sector to produce state-of-the-art therapeutics for societal needs whilst respecting the finite resources provided by the environment.

Advances in Drug Design

Prominent advances in drug design are reliant on chemical synthesis platforms allowing the efficient exploration of chemical space to discover next-generation functional molecules. As a result, innovation is currently limited by the practical implementation of enabling methods, which often becomes the rate-limiting factor in cutting-edge research. This limitation is more pronounced when translating academic research to industrial settings.

Opportunity for Sustainability

The current renaissance of organic photochemistry and light-driven processes, in a broader sense, provides an opportunity to reconcile the growing demand for new functional molecules with consideration of sustainability and atom economy.

Project Overview: LUMIBOR

Inspired by the importance of organoboron motifs in medicinal chemistry, this EU action “LUMIBOR” will harness the untapped potential of boron hybridization and boron ligand design to unlock new excited state reactivity paradigms. This initiative aims to facilitate the discovery of new methods to access achiral and chiral 3D organoboron scaffolds.

Structural Platform Development

LUMIBOR will create a structural platform to utilize boron hybridization in the development of next-generation light-enabled ACTIVATION methods. Understanding the correlation between hybridization and parameters such as excited state energy and adjacent bond dissociation energy will allow access to synthetically versatile, high-energy intermediates such as:

1. α-boryl radicals
2. The triplet excited state

Strategic Control Over Reactivity

Strategic control over boron hybridization will also be utilized to regulate reactivity by influencing:

• Radical philicity
• Spin density
• Excited state lifetimes
• Other parameters

Conclusion

Collectively, LUMIBOR will create expansive guidelines to expand the synthesis arsenal by developing novel platforms to construct desirable 3D organoboron molecules.