Summary
The late-stage functionalization (LSF) of bioactive compounds is currently a hot topic in the chemistry community, as it allows for the rapid and divergent construction of molecule complexity and avoids the need for time-consuming de novo synthesis. This is especially relevant in the fields of drug discovery and medicinal chemistry where the fast identification of structure-activity relationships is crucial. Especially intriguing in this context are alkenes and 1,3-dienes, as they are frequently occurring motifs in natural products and drug molecules including important antibiotics and antivirals. However, methods for the introduction of a broad variety of functional groups via the LSF of these moieties remain underdeveloped. LateFun aims to create new chemical space by developing a first-in-class methodology for the incorporation of a highly versatile functional handle via the LSF of alkenes and 1,3-dienes, whose well-established subsequent transformations will allow for the rapid assembly of diverse structures. Applying this innovative protocol to the LSF of complex natural products and drug molecules will be of great importance and impact, going beyond the current state of art. The real-life applications of this cutting-edge research proposal will be explored during a secondment phase in Novartis (Basel), providing for valuable industry insights and interdisciplinary aspects. The host’s expertise in late-stage functionalization of bioactive molecules using catalytically generated carbyne equivalents perfectly complements the applicant’s strong background in photocatalysis and therefore guarantees two-way-transfer of knowledge between the host group and the ER (Experienced Researcher). The successful implementation of this action in the highly international and interdisciplinary environment of ICIQ and Novartis will enable the fellow to develop a unique research profile and will be crucial in building an independent academic career.
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More information & hyperlinks
Web resources: | https://cordis.europa.eu/project/id/101152204 |
Start date: | 01-09-2025 |
End date: | 31-08-2027 |
Total budget - Public funding: | - 165 312,00 Euro |
Cordis data
Original description
The late-stage functionalization (LSF) of bioactive compounds is currently a hot topic in the chemistry community, as it allows for the rapid and divergent construction of molecule complexity and avoids the need for time-consuming de novo synthesis. This is especially relevant in the fields of drug discovery and medicinal chemistry where the fast identification of structure-activity relationships is crucial. Especially intriguing in this context are alkenes and 1,3-dienes, as they are frequently occurring motifs in natural products and drug molecules including important antibiotics and antivirals. However, methods for the introduction of a broad variety of functional groups via the LSF of these moieties remain underdeveloped. LateFun aims to create new chemical space by developing a first-in-class methodology for the incorporation of a highly versatile functional handle via the LSF of alkenes and 1,3-dienes, whose well-established subsequent transformations will allow for the rapid assembly of diverse structures. Applying this innovative protocol to the LSF of complex natural products and drug molecules will be of great importance and impact, going beyond the current state of art. The real-life applications of this cutting-edge research proposal will be explored during a secondment phase in Novartis (Basel), providing for valuable industry insights and interdisciplinary aspects. The host’s expertise in late-stage functionalization of bioactive molecules using catalytically generated carbyne equivalents perfectly complements the applicant’s strong background in photocatalysis and therefore guarantees two-way-transfer of knowledge between the host group and the ER (Experienced Researcher). The successful implementation of this action in the highly international and interdisciplinary environment of ICIQ and Novartis will enable the fellow to develop a unique research profile and will be crucial in building an independent academic career.Status
SIGNEDCall topic
HORIZON-MSCA-2023-PF-01-01Update Date
17-11-2024
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