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New late-stage functionalization reagents for the construction of chiral centers to impact drug discoveryhis her

Objective

Late-stage functionalization (LSF) is a rapidly expanding field in molecular synthesis with the major goal of quickly accessing to derivatives that would be too challenging or time-consuming to prepare otherwise; hence, this strategy has a great potential to impact drug discovery processes by speeding up the hit-to-lead optimization. At present, more than two-thirds of prescription drugs contain at least one chiral center. However, the late-stage introduction of this structural motif using aromatic CH bonds is an enduring challenge in synthesis. The goal of the NAKED-C project is to develop a new methodology for the construction of chiral centers in drug molecules, relying on the design and synthesis of a novel class of atomic carbon precursors that, upon successive and appropriate activations, would allow to build tailored asymmetric carbons. To achieve this goal, a new visible-light photoredox catalytic diazomethylation of aromatic CH bonds will be developed. The collaboration with an industrial partner (secondment at AiCuris) will allow the application of this novel strategy to drug discovery in the search of effective antibiotics, thus merging multidisciplinary aspects with intersectoral knowledge transfer. The result will be a brand-new assembly point for the construction of chiral centers in bioactive compounds, with the potential to become a late-stage diversity-generating synthetic platform for drug discovery programs. The proposal merges the host expertise in novel CH functionalization strategies based on photocatalysis, and the researchers background in classical radical chemistry, metal-mediated synthesis and pharmacology, ensuring the two-way transfer of knowledge between the fellow and the host group. Successful development of NAKED-C will enhance the scientific and transferable skills of the researcher, while forthcoming to the fellows professional goal of pursuing an independent research career in academia in synthetic organic chemistry.

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Keywords

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Programme(s)

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Topic(s)

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Funding Scheme

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HORIZON-TMA-MSCA-PF-EF - HORIZON TMA MSCA Postdoctoral Fellowships - European Fellowships

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Call for proposal

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(opens in new window) HORIZON-MSCA-2022-PF-01

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Coordinator

FUNDACIO PRIVADA INSTITUT CATALA D'INVESTIGACIO QUIMICA
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 181 152,96
Address
AVENIDA PAISSOS CATALANS 16
43007 TARRAGONA
Spain

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Region
Este Cataluña Tarragona
Activity type
Research Organisations
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Total cost

The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.

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