Objective
Research objectives and content
The objectives of the present proposal are the total synthesis of martinelline and martinellic acid, two alkaloids with a triciclic core of pyrrolo(3,2-c)quinolone system that had not been reported previously in any natural product. Both alkaloids were isolated in 1995 from the root of Martinella iquitosensis for Merck laboratory and show bradykinin B 1 and B2 receptor antagonist activity in studies made for a group at Merck. This year the group of Dr. Jones have started the synthesis of both alkaloids and recently has published a short, high-yielding synthesis of the tricyclic pyrroliquinoline core of martinelline. The key step of this synthesis was the radical cyclisation of an aryl radical onto a pyrrole ring. The present proposal calls for extending this radical cyclisation into a total synthesis of these interesting natural products, firstly in a racemic way and secondly in a enantiopure form. The successful completion of this project will represent an important step forward in the use of aryl radical chemistry in natural products synthesis and would open the way to the preparation of analogues of martinelline with enhanced biological activity.
Training content (objective, benefit and expected impact)
This project will provide excellent training in modern synthetic organic chemistry. It involves radical chemistry, organometallic chemistry and modern heterocyclic chemistry all carried out against the challenge of the synthesis of an unusual and interesting natural product. Chemist with expertise and training in this area are much sought after by the pharmaceutical and agrochemical industries.
Links with industry / industrial relevance (22)
The synthesis of martinelline and some of their analogues will be of significant interest to pharmaceutical companies and it is intended to use the strong links already in place via the host group to develop links with suitable companies. For example, intermediate compounds and any analogues synthesized will be submitted for biological testing at appropiate companies. These results could be of significant interest and may lead to the development of a new pharmaceutical product.
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.
- natural sciences chemical sciences organic chemistry
- medical and health sciences basic medicine pharmacology and pharmacy pharmaceutical drugs
- natural sciences chemical sciences inorganic chemistry organometallic chemistry
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Programme(s)
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Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Topic(s)
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.
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.
Call for proposal
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Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
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.
Coordinator
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.