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Chirality via Cross Coupling New Asymmetric C C Bond Formations Driven by Atom...

Chirality via Cross Coupling New Asymmetric C C Bond Formations Driven by Atom and Step Economy Over 60% of the world’s top selling small molecule drug compounds are chiral and, of these, approximately 80% are marketed as single enantiomers. Surprisingly, and despite the tremendous advances made in catalysis over the past se... ver más

31/08/2025

THE UNIVERSITY OF...

2M€

Presupuesto del proyecto: 2M€

Líder del proyecto

THE UNIVERSITY OF LIVERPOOL No se ha especificado una descripción o un objeto social para esta compañía.

TRL 4-5

Ver 2 Participantes

Financiación concedida El organismo H2020 notifico la concesión del proyecto el día 2020-03-03

ERC-2019-COG: ERC Consolidator Grant

I+D

Cerrada hace 5 años

0% 100% 100%

2 Participantes

THE UNIVERSITY OF LIVERPOOL

2.00M€ | Lider

NOSCIRA

1.15M€ | Participante

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Duración del proyecto: 65 meses Fecha Inicio: 2020-03-03
Fecha Fin: 2025-08-31

Líder del proyecto

THE UNIVERSITY OF LIVERPOOL No se ha especificado una descripción o un objeto social para esta compañía.

TRL 4-5

Presupuesto del proyecto 2M€

Descripción del proyecto Over 60% of the world’s top selling small molecule drug compounds are chiral and, of these, approximately 80% are marketed as single enantiomers. Surprisingly, and despite the tremendous advances made in catalysis over the past several decades, the average chiral complexity of drug discovery libraries has actually decreased, while, at the same time the chiral complexity of marketed drugs has increased. Consequently, there is now an urgent need to provide efficient processes that access directly privileged chiral 3D building blocks. It is our philosophy that catalysis holds the key here and new processes should be based upon atom and step economical platforms that exert control over both absolute and relative stereochemistry. Palladium catalysed cross-coupling reactions of aryl (pseudo)halides with organo-nucleophiles (esp. the Suzuki coupling) have become mainstays of the pharmaceutical industry. Here, multiple concession steps are usually required to prepare the reaction partners, thereby detracting from atom and step economy. Further, these processes predominantly provide planar 2D structures and are not well suited to the production of chiral 3D building blocks. Consequently, methods that allow feedstock precursors (e.g. alkenes and aryl C-H bonds) to be combined directly in enantioselective or enantiospecific C-C bond formations are highly desirable. Cross-couplings of this type would circumvent concession steps, thereby minimising cost, effort and waste; however, such processes are highly challenging because of issues associated with regio- and stereocontrol. Recently, we developed prototype catalyst systems that can address this. In the proposed ERC project, these exciting preliminary results will be developed into a wider family of processes where asymmetric C-C bond formations are achieved directly by C-H activation. The new methods, which fulfil modern reaction ideals of atom and step economy, will likely find broad use in applied settings.

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