Publications associées à Head‐to‐Tail Dimerization of N‐Heterocyclic Diazoolefins

Functionalization of harmonic nanoparticles for drug release and multimodal imaging applications

Cancer is among the leading causes of death worldwide, and as knowledge of the disease continues to grow there is an increasing interest towards precision medicine: more specifically towards the theranostics field, i.e the development of targeted molecular ...

EPFL2024

Synthesis and application of bifunctional hypervalent iodine reagents for peptide modification

Elija Grinhagena

Protein-protein interactions (PPIs) are responsible for regulating many biological processes in human bodies. PPIs often have a large binding site and often interact through an alpha helical segment. Therefore, the inhibition of PPIs can be difficult using ...

EPFL2023

Development of remote C-H bond functionalization of redox-active alcohol derivatives and oxidative transformations under photoredox catalysis

Alexandre Julien Florent Leclair

The development of radical-based remote C(sp3)-H functionalizations of redox-active alcohol derivatives, oxidative cycloaddition and rearrangement transformations under visible light photocatalysis constitute the basis of this thesis. The first chapter des ...

EPFL2021

Isolation and characterization of diazoolefins

Kay Severin, Rosario Scopelliti, Farzaneh Fadaei Tirani, Paul Varava, Zhaowen Dong

Diazoolefins tend to be highly reactive compounds that rapidly lose dinitrogen. So far, most experimental evidence for diazoolefins is indirect, via trapping experiments. Here we show that diazoolefins are observed to form in reactions of N-heterocyclic ol ...

2021

Copper-Catalyzed 1,2-Methoxy Methoxycarbonylation of Alkenes with Methyl Formate and Synthetic Studies Towards the Total Synthesis of Koumine, Voacafricine A and Voacafricine B

Balázs Budai

The development of an unusual oxidative alkene difunctionalization using methyl formate and syn-thetic studies towards alkaloid natural products provide the basis of the thesis. The first chapter details the development of a method that forges methoxycarbo ...

EPFL2020

Development of Photocatalysts towards the Visible-Light driven C-Terminal Bioconjugation of Peptides and Proteins

Marion Marie-Agnès Garreau

If small molecules have led to tremendous progress in curing diseases, new therapeutic agents such as peptides or antibody-drugs conjugates have emerged as a highly promising next generation of pharmaceuticals. As for small molecules, their derivatization ...

EPFL2020

Nitrogen-doped graphene stabilized copper nanoparticles for Huisgen [3+2] cycloaddition "click" chemistry

Yves Leterrier, Véronique Michaud, Monika Srivastava, Sravendra Rana

Nitrogen-doped reduced graphene oxide (NRGO) stabilized copper nanoparticles are designed to assist Cu(I)-catalyzed Huisgen [3+2] cycloaddition "click" chemistry (CuAAC). This study demonstrates a robust route for the synthesis of vastly dispersed heteroge ...

Royal Society of Chemistry2019

Investigations of the Chemistry of 1-Alkynyltriazenes

Florian Gérald Abela

The chemistry of aromatic triazenes is well known, and has been explored for more than a century. These compounds have emerged as very useful intermediates, because of their unique reactivity. This functionality can notably be used to access many other fun ...

EPFL2018

Can Biomimetic Zinc Compounds Assist a (3 + 2) Cycloaddition Reaction? A Theoretical Perspective

Ursula Röthlisberger, Esra Bozkurt

Compounds bearing tetrazole rings are valuable facets in numerous branches of chemistry including metabolic imaging and the production of drugs and high-energy materials. Synthesis of tetrazoles with the help of organocatalysts has intensively been explore ...

2017

Switchable [3+2] and [4+2] Heteroannulation of Primary Propargylamines with Isonitriles to Imidazoles and 1,6-Dihydropyrimidines: Catalyst Loading Enabled Reaction Divergence

Qian Wang, Jieping Zhu, Shuo Tong

Isonitrile 1 due to its carbene-like reactivity serves generally as a one-carbon synthon in a diverse set of organic transformations. We report in this article that the isocyano group can also act as a polarized triple bond to undergo, as a two-atom syntho ...

Wiley-Blackwell2016

Site-Specific Glycoconjugation of Protein via Bioorthogonal Tetrazine Cycloaddition with a Genetically Encoded trans-Cyclooctene or Bicyclononyne

Lin Xue

Efficient access to proteins modified site-specifically with glycans is important in glycobiology and for therapeutic applications. Herein, we report a biocompatible protein glycoconjugation by inverse demand Diels-Alder reaction between tetrazine and tran ...

American Chemical Society2015

Potential of Cycloaddition Reactions To Generate Cytotoxic Metal Drugs In Vitro

Paul Joseph Dyson, Stéphanie Crot, Benjamin Samuel Murray, Sviatlana Siankevich

Severe general toxicity issues blight many chemotherapeutics utilized in the treatment of cancers, resulting in the need for more selective drugs able to exert their biological activity at only the required location(s). Toward this aim, we report the devel ...

Amer Chemical Soc2014

Peptide/protein – polymer conjugates: synthetic strategies and design concepts

Harm-Anton Klok, Marc Gauthier

This feature article provides a compilation of tools available for preparing well-defined peptide/protein–polymer conjugates, which are defined as hybrid constructs combining (i) a defined number of peptide/protein segments with uniform chain lengths and d ...

Royal Society of Chemistry2008

Fluoronaphthalene building blocks via arynes: A solution to the problem of positional selectivity

Eric Masson

When 3-fluoro- and 3-chloro-1,2-didehydrobenzenes are generated in the presence of 2-(trimethylsilyl)furan, two regioisomeric cycloadducts are formed in a 1:2 ratio. However, regioselectivity can be installed by fitting one bulky trimethylsilyl group into ...

2005