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Grant: Collaborative Research and Development Grants

Simon Fraser University

$160,000.00

Direct 19F- and 18F- fluorination of heterocycles for medicinal chemistry and radiotracer synthesis

EF 2018-19

Résumé
Fluorine is the 13th most abundant element on earth, and exists primarily in mineral compositions in the earths crust. It is not commonly used by living systems, but this element has found many uses in organic chemistry, due to the strength of the C-F bond, and organofluorine compounds - compounds that contain a C-F bond - are commonly used as refrigerants, electric insulants and cookware (as PTFE). Another major role for organofluorine compounds is in drugs, where placing a single fluorine atom in the correct position on a pharmaceutical can have major and desireable impact on the biological properties of the molecule. Of all commercialized drugs, approximately 20% contain fluorine, including important drugs in various classes. Furthermore, an unstable isotope of fluorine, F-18, is routinely used for positron emission tomography (PET) imaging, a technique that allows clinicians to examine biochemical processes such as cancer cell growth in a live subject. However, despite the importance of fluorine in pharmaceuticals and medicine, it is still difficult to place a fluorine atom in a specific position of a molecule. The Britton group at SFU, in collaboration with F. Hoffmann LaRoche - one of the largest pharmaceutical companies in the world - has developed several methods to introduce a fluorine atom into a molecule under gentle conditions. This has enabled the creation of novel fluorinated molecules, including F-18 labeled molecules that can detect cancerous tumors in mice via PET imaging. This research project aims to expand the methods available to biomedical researchers to quickly and gently introduce a fluorine atom into drug molecules for the purpose of optimizing their properties, or for the purposes of creating new PET imaging agents.
Programme
Collaborative Research and Development Grants
Emplacement
British Columbia, Canada
Type de bénéficiaire
Academia
Type
Grant
Source
NSERC's Awards Data

Tel que publié

Application id
520227-2017
Name nom
Britton, Robert
Department département
Chemistry
Organization id
5
Institution établissement
Simon Fraser University
Province en
British Columbia
Province fr
Colombie-Britannique
Country en
CANADA
Country fr
CANADA
Fiscal year exercice financier
2018
Competition year année de concours
2017
Award amount
160000
Program id
CRDPJ
Program name en
Collaborative Research and Development Grants
Program name fr
Subventions de recherche et développement coopérative
Group en
Research partnerships programs
Group fr
Programmes de partenariat
Committee code
96
Committee name en
RPP Internal Decision Cttee
Committee name fr
Cté de décision interne - PPR
Area of application code
504
Area of application group en
Manufacturing processes and products
Area of application group fr
Procédés et produits industriels
Area of application en
Human pharmaceuticals
Area of application fr
Produits pharmaceutiques administrables à l'homme
Research subject code
3703
Research subject group en
Organic chemistry
Research subject group fr
Chimie organique
Research subject en
Organic syntheses
Research subject fr
Synthèses organiques
Partie
1
Nb partie
2
Application title
Direct 19F- and 18F- fluorination of heterocycles for medicinal chemistry and radiotracer synthesis
Keyword
NSERC
Application summary
Fluorine is the 13th most abundant element on earth, and exists primarily in mineral compositions in the earths crust. It is not commonly used by living systems, but this element has found many uses in organic chemistry, due to the strength of the C-F bond, and organofluorine compounds - compounds that contain a C-F bond - are commonly used as refrigerants, electric insulants and cookware (as PTFE). Another major role for organofluorine compounds is in drugs, where placing a single fluorine atom in the correct position on a pharmaceutical can have major and desireable impact on the biological properties of the molecule. Of all commercialized drugs, approximately 20% contain fluorine, including important drugs in various classes. Furthermore, an unstable isotope of fluorine, F-18, is routinely used for positron emission tomography (PET) imaging, a technique that allows clinicians to examine biochemical processes such as cancer cell growth in a live subject. However, despite the importance of fluorine in pharmaceuticals and medicine, it is still difficult to place a fluorine atom in a specific position of a molecule. The Britton group at SFU, in collaboration with F. Hoffmann LaRoche - one of the largest pharmaceutical companies in the world - has developed several methods to introduce a fluorine atom into a molecule under gentle conditions. This has enabled the creation of novel fluorinated molecules, including F-18 labeled molecules that can detect cancerous tumors in mice via PET imaging. This research project aims to expand the methods available to biomedical researchers to quickly and gently introduce a fluorine atom into drug molecules for the purpose of optimizing their properties, or for the purposes of creating new PET imaging agents.