PHOTO-FLUOR | Enantioselective Carbon-Fluorine Bond Formation: A Molecular Editing Approach toward Drug Discovery

Summary
The unique properties of the carbon-fluorine (C-F) bond explain why organofluorine compounds play a central role in biopharmaceuticals. One current challenge in drug discovery is the selective installation of C-F stereogenicity within the active site of lead candidates, such molecular editing may greatly help in increasing potency and understanding metabolic degradation paths. However, the limited C-F bond formation techniques complicate this approach and providing new versatile catalytic techniques, which can expand the substrate pool amenable to C-F bond formation, would greatly boost the impact of fluorine chemistry in drug discovery. We aim at developing methods that require feedstock materials as substrates, such as alkene and alkane derivatives. The new methods will combine the potential of enantioselective organocatalysis or metal-mediated processes with visible light photocatalysis.
The PHOTO-FLUOR project is unique in that it provides training in “enantioselective fluorination” and “catalysis applied to drug discovery”, areas that contribute to European excellence. The resulting techniques may immediately impact the EU Health sector.
PHOTO-FLUOR will merge the expertise of the host group in photochemical enantioselective reactions with the background of the applicant in transition metal catalysis, to reach the desired deliverables and milestones. In addition, a secondment at an internationally recognized pharma-company has been included in the work plan for conducting biological study of the fluorine-edited bioactive molecules. The applicant will transfer knowledge to both host groups creating a link between them to forge future collaborations. Finally, an ambitious training program, which includes a number of new scientific and soft skills to be transferred to the applicant, is also envisaged. The multi-cultural nature of this project will greatly broaden the fellow competencies and will place him in an excellent position for the next career move.
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More information & hyperlinks
Web resources: https://cordis.europa.eu/project/id/796460
Start date: 09-05-2018
End date: 08-05-2020
Total budget - Public funding: 170 121,60 Euro - 170 121,00 Euro
Cordis data

Original description

The unique properties of the carbon-fluorine (C-F) bond explain why organofluorine compounds play a central role in biopharmaceuticals. One current challenge in drug discovery is the selective installation of C-F stereogenicity within the active site of lead candidates, such molecular editing may greatly help in increasing potency and understanding metabolic degradation paths. However, the limited C-F bond formation techniques complicate this approach and providing new versatile catalytic techniques, which can expand the substrate pool amenable to C-F bond formation, would greatly boost the impact of fluorine chemistry in drug discovery. We aim at developing methods that require feedstock materials as substrates, such as alkene and alkane derivatives. The new methods will combine the potential of enantioselective organocatalysis or metal-mediated processes with visible light photocatalysis.
The PHOTO-FLUOR project is unique in that it provides training in “enantioselective fluorination” and “catalysis applied to drug discovery”, areas that contribute to European excellence. The resulting techniques may immediately impact the EU Health sector.
PHOTO-FLUOR will merge the expertise of the host group in photochemical enantioselective reactions with the background of the applicant in transition metal catalysis, to reach the desired deliverables and milestones. In addition, a secondment at an internationally recognized pharma-company has been included in the work plan for conducting biological study of the fluorine-edited bioactive molecules. The applicant will transfer knowledge to both host groups creating a link between them to forge future collaborations. Finally, an ambitious training program, which includes a number of new scientific and soft skills to be transferred to the applicant, is also envisaged. The multi-cultural nature of this project will greatly broaden the fellow competencies and will place him in an excellent position for the next career move.

Status

CLOSED

Call topic

MSCA-IF-2017

Update Date

28-04-2024
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Horizon 2020
H2020-EU.1. EXCELLENT SCIENCE
H2020-EU.1.3. EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions (MSCA)
H2020-EU.1.3.2. Nurturing excellence by means of cross-border and cross-sector mobility
H2020-MSCA-IF-2017
MSCA-IF-2017