Objective
Enantiopure quaternary amino acids, carrying two carbon-based substituents at the α carbon, are one of the most important groups of modified α amino acids, of great commercial value in the development of new pharmaceuticals and agrochemicals. Certain of these quaternary amino acids are readily available by stereoselective α alkylation of available amino acids, but not those functionalized by the addition of α-aryl groups. In this project, we propose to develop an industrially scalable, practical method for the synthesis of α-arylated quaternary amino acids in enantiomerically pure form by streamlining, optimization and scale-up of a reaction we discovered while working on the synthesis of quaternary amino acids as conformational controllers within an ERC-funded Advanced Grant. The method is operationally simple and employs only inexpensive commodity chemicals as precursors. It uses no chiral auxiliary or catalyst, and exploits both structure and stereochemistry of the starting amino acid to make the quaternary amino acids in enantiomerically pure form. It avoid the use of transition metals, freeing the method from the potential problems associated with their toxicity, cost and volatility of supply. The nearest competitive methods are either limited in scope to electron-deficient aryl rings, or they employ toxic and expensive transition metal catalysts. Interest in the method has been garnered from the fine chemical, pharmaceutical and agrochemical industry, but further work on scale-up and practical issues are needed for the technology to become industry-ready.
In parallel with this main thrust of the project, we will carry out preliminary work on related chemistry, developing a new, simple route to analogues of arogenate into a practical method for the synthesis of a new agrochemical targets of potentially very great commercial interest. The ready availability of these compounds will offer significant potential for future agrochemical innovation.
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 pharmaceutical drugs
- natural sciences chemical sciences catalysis
- natural sciences chemical sciences organic chemistry amines
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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.
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H2020-EU.1.1. - EXCELLENT SCIENCE - European Research Council (ERC)
MAIN PROGRAMME
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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.
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.
ERC-POC - Proof of Concept Grant
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Call for proposal
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
(opens in new window) ERC-2016-PoC
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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.
BS8 1QU BRISTOL
United Kingdom
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.