La maladie d'Alzheimer et la place des polyphénols au sein des nouvelles stratégies thérapeutiques (analyse multi-techniques des intéractions "polyphénols-peptide tau")

LIMOGES-BU Médecine pharmacie (870852108) / SudocLYON1-BU Santé (693882101) / SudocSudocFranceF

Développement d'outils organométalliques en vue du transfert de méthyle, application à la synthèse de radiotraceurs pour la TEP

Le couplage de Stille modifié développé par l équipe du Pr Fouquet a été appliqué à la méthylation de nucléosides, dinucléotides et oligonucléotides dans le but de mettre au point une méthodologie de marquage d aptamères au carbone 11 pour le diagnostic précoce de cancer par TEP. Ce couplage pallado-catalysé est basé sur l utilisation de monoorganoétain activé par une source de fluorure permettant d accélérer la réaction. Dans un premier temps, les essais méthodologiques ont permis de mettre au point le transfert de groupement méthyle sur différents nucléosides et un dinucléotide modifiés dans des conditions compatibles avec la durée de demi-vie du carbone 11 (20,4 min) et la nature particulière des oligonucléotides. Puis, cette méthodologie a été appliquée à des oligonucléotides modèles obtenus après incorporation des nucléosides les plus prometteurs.The modified Stille cross-coupling developed by Pr. Fouquet s group was applied to the methylation of nucleosides, dinucleotides and oligonucleotides in order to develop a methodology for labelling aptamers with carbon 11 for the early diagnosis of cancer by PET. This pallado-catalyzed cross-coupling is based on the use of monoorganotin activated by a source of fluoride accelerating the reaction. Initial methodology tests helped to finalize the transfer of methyl group on various nucleosides and a dinucleotide, with reaction conditions compatible with the short half-life of carbon 11 (20.4 min) and the special nature of oligonucleotides. Then, this methodology was applied to oligonucleotide models obtained after incorporation of the most promising nucleosides.BORDEAUX1-Bib.electronique (335229901) / SudocSudocFranceF

Epigallocatechin 3-Gallate as an Inhibitor of Tau Phosphorylation and Aggregation: A Molecular and Structural Insight

International audienc

Palladium-catalyzed cascade allylation/carbopalladation/cross coupling: a novel three-component reaction for the synthesis of 3,3-disubstituted-2,3-dihydrobenzofurans

International audienc

From the gold-catalysed benzylation of arenes to the regio- and stereoselective synthesis of procyanidins dimers

International audienc

Pd0-Catalyzed Methyl Transfer on Nucleosides and Oligonucleotides, Envisaged as a PET Tracer

The methyl transfer reaction from activated monomethyltin, via a modified Stille coupling reaction, was studied under “ligandless” conditions on fully deprotected 5'-modified nucleosides and one dinucleotide. The reaction was optimized to proceed in a few minutes and quantitative yield, even under dilute conditions, thus affording a rapid and efficient new method for oligonucleotide labelling with carbon-11

Palladium-Catalyzed Heterocyclization:A Carbon-Centered Approach

Heterocycles are some of the most important and widely used motifs in synthetic and medicinal chemistry. It is therefore not surprising that the synthesis of heterocycles is a rich area of chemistry. Catalytic heterocyclisation that makes use of heteroatom nucleophiles such as oxygen and nitrogen is one such powerful strategy. This Focus Review considers an alternative approach using carbon-based nucleophiles generated during palladium-catalysed heterocyclisation. This complimentary method allows access to a range of useful and otherwise inaccessible targets. Occurring through a range of different mechanisms, the utility of this approach can be seen in the wide range of transformations that can be undertaken, along with its repeated application in complex molecule synthesis