Objective
The aim of this project is the development of new approaches to aza-bioactive targets. In particular, the synthesis of b-,g- and d-lactams with the emphasis on (lactam-derived antibiotics is planned. The strategy to be developed is based on previous results about N-alkylidene-bis(trimethylsilyl)methylamines as a new series of stable imines. These imines on treatment with aminoketene synthons and further chemical elaboration of the resulting cycloadducts should provide a route to monobactams and related, b-lactam antibiotics.
The first step of the synthesis will be performed by using the Evans-Sjogren ketenes, but other aminoketene synthons derived from ty- and o-lactams will also be studied to improve the stereochemical course of the cycloaddition reaction. The g- and d-lactams will be prepared through substitution reactions carried out on the corresponding N-trimethylsilyl and N-[(chlorodimethylsilyl)methyl]-lactams. The synthesis of lactamopeptides and N-methyl a-amino acids from these lactams will also be explored in conjunction with a route to b-lactamoketones.
In parallel with these approaches to a-amino acids and related derivatives, the synthesis of a-amino acid-N-carboxy anhydrides from b-lactams is also envisaged. The reaction sequence consists of a a-hydroxylation of the corresponding a-amino b-lactam followed by Baeyer-Villiger oxidation of the resulting a-keto-b-lactam
Fields of science (EuroSciVoc)
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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.
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.
Call for proposal
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Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
Funding Scheme
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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.
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Coordinator
20080 San Sebastian
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.