COMBICHEM-GIRONA · Synthesis of pyrimidine and spiroimidazolidinone libraries by combinatorial chemistry
FP6 — Marie Curie Actions (Human Resources and Mobility)
- Duration
- 2004-03-01 → 2005-02-28
- EU contribution
- €40,000
- Participants
- 1
- Scheme
- ERG
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Results in brief
Final Activity Report Summary - COMBICHEM-GIRONA (Synthesis of pyrimidine and spiroimidazolidinone libraries by combinatorial chemistry)
In this project, an efficient methodology has been developed for the synthesis of novel pyrimidines substituted at position 2 and / or 4 with an amino acid residue. We incorpored N-Boc-amino esters with an amine, hydroxyl, heteroaryl or phenol group in the side-chain at 2 position of the pyrimidine ring by nucleophilic displacement of a sulphone function. Two different strategies based on Mitsunobu and Petasis reaction were performed to introduce an amino ester residue at 4 position of the pyrimidine ring. On the other hand, we set up a methodology for the rapid and efficient solid-phase synthesis of spiroimidazolidinones, in particular, of novel 1,4,8-triazaspiro[4.5]decan-2-one derivatives. We optimised the preparation of 1,4,8-triazaspiro[4.5]decan-2-one-1-acetamides substituted at 4 and 8 positions as well as the preparation of 4-aryl-8-benzyl-1,4,8-triazaspiro[4.5]decan-2-ones substituted at position 1. Both optimization studies were performed by the Multipin technology using SynphaseTM Lanterns as solid support. This methodology was used for the preparation of a collection of novel spiroimidazolidinone derivatives.
Data: CORDIS, © European Union
Project objective
I will be reintegrated in a research group (the Organic Synthesis Group of the University of Girona) different from my PhD group and in my country of origin (Spain). My reintegration will be achieved by managing a project that involves two parts. The first part will allow me the incorporation in this group. The second part will promote starting an international cojlaboration between this Spanish group and the French group in which I hold the Marie Curie Fellowship during my post-doctoral period. Thus, inter national scientific exchanges and mobility will be established. The first part is a continuation of a current project in the Organic Synthesis Group. It is based on the synthesis of pyrimidine libraries. The expertise of this group in pyrimidine synthesis will be combined with my expertise in combinatorial chemistry acquired in my post-doctoral period. The second part is centered on the preparation of spiroimidazolidinone libraries and is a continuation of the project I developed as Marie Curie Fellow. The development of this project will allow me to apply the knowledge on heterocyclic and solution chemistry acquired in my PhD, and also my expertise in solid phase and combinatorial chemistry, specially the Multipin technology, acquired during the Marie Curie Fellowship. The expertise of the Organic Synthesis Group in solid-phase chemistry will offer me the opportunity of continuing the training in solid-phase chemistry that I initiated in the postdoctoral period. Specially, I will learn the use of resins. Hol ding this ERG will offer me the possibility of being integrated in an academic environment in addition to developing a scientific career. The University of Girona assures an effective and lasting reintegration as assistant professor of organic chemistry.
Original text from CORDIS.
Participants
- UNIVERSITAT DE GIRONA · GERONACoordinatorSpain
Links
Data: CORDIS, © European Union