Project description
A new method of housane production could transform drug design and medicinal chemistry
Cyclopropanes and cyclobutanes are small ring structures commonly used in drug molecules because they improve how drugs behave in the body. However, a unique structure that combines these two rings, called housane, has been largely unexplored mainly owing to the lack of efficient methods for its synthesis. With the support of the Marie Skłodowska-Curie Actions programme, the Housane project plans to develop a new method to construct housanes using a chemical process called Rh-catalysed carbyne transfer. The proposed approach will make it easier and more sustainable to create housanes, which could lead to new drug discoveries. Researchers will collaborate with a pharmaceutical company to test real-world applications.
Objective
Aliphatic sp3-rich ring systems such as cyclopropanes and cyclobutanes are commonly observed motif in drug molecules. This is due to the fact that they can positively influence metabolic stability, conformation, pKa, entropy, membrane permeability or pharmacokinetics in drug leads. However, the molecule consists of a cyclopropane fused to cyclobutane, traditionally known as ‘housane’ is significantly underexplored and yet to appear in drug molecules. This can largely be attributed to the lack of general synthetic methods for the preparation of this motif. Current protocols for the synthesis of housane, require multistep manipulations or pre-functionalized substrates, which means low efficiency and sustainability. Housane aims to develop an innovative technology to rapidly construct housanes and housane derivative of drug molecules from feedstock and fine alkenes based on a Rh-catalyzed carbyne transfer platform. A key strength of this conceptually new and multidisciplinary proposal is the introduction of a secondment phase in Janssen (Toledo, Spain) to explore real-life applications. The ambitious action merges perfectly with the expertise of the host in novel C-H and C–C bond functionalization strategies based on the catalytic generation of carbyne equivalents with the strong background of the applicant in transition metal-catalyzed asymmetric allylic substitution chemistry, thus enhancing two-way transfer of knowledge between the ER and the host group. This project will expose the fellow to a wide range of cutting-edge chemistry including medicinal chemistry in an interdisciplinary and international environment (ICIQ, Janssen) and enable the fellow to become a leader for the next generation in the field of organic synthesis, homogeneous catalysis and medicinal chemistry.
Fields of science (EuroSciVoc)
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
- medical and health sciences basic medicine pharmacology and pharmacy pharmacokinetics
- natural sciences chemical sciences catalysis
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Keywords
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Programme(s)
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
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HORIZON.1.2 - Marie Skłodowska-Curie Actions (MSCA)
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Topic(s)
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Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Funding Scheme
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
HORIZON-TMA-MSCA-PF-EF - HORIZON TMA MSCA Postdoctoral Fellowships - European Fellowships
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Call for proposal
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Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
(opens in new window) HORIZON-MSCA-2024-PF-01
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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.
43007 Tarragona
Spain
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.