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HALODRUGSYN SIGNED

Innovative Strategies towards Halogenated Organic Molecules: From Reaction Design to Application in Drug Synthesis

Total Cost €

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EC-Contrib. €

0

Partnership

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 Outcomes and results

 HALODRUGSYN project word cloud

Explore the words cloud of the HALODRUGSYN project. It provides you a very rough idea of what is the project "HALODRUGSYN" about.

create    strategies    achievements    synthetic    bacterial    unparalleled    efficient    drug    natural    setting    strains    chemistry    activation    reactions    valuable    halogen    equipped    heteroarene    units    prevent    lack    expertise    resistance    time    heteroarenes    bond    realization    antibiotics    manner    extend    solution    strategy    synthesis    precision    selectivity    confident    platform    transformations    elaborated    groundbreaking    expansion    salimabromide    structural    halogenated    motifs    combat    construction    carbon    toolbox    record    molecular    pharmaceutical    cancer    bonds    broadly    acute    outstanding    chemotherapeutics    resistant    ring    am    infections    applicable    innovative    synthesized    constitute    with    fluorine    installation    first    restrictions    fluorinated    practicability    industry    limitations    drugs    publication    unprecedented    efficiency    functional    antibiotic    arenes    anti    engineering    gained    provides    goals   

Project "HALODRUGSYN" data sheet

The following table provides information about the project.

Coordinator		 UNIVERSITAET INNSBRUCK 

Organization address
address: INNRAIN 52
city: INNSBRUCK
postcode: 6020
website: http://www.uibk.ac.at

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.
 Coordinator Country Austria [AT]
 Project website https://www.uibk.ac.at/organic/magauer/index.html.en
 Total cost 1˙496˙664 €
 EC max contribution 1˙496˙664 € (100%)
 Programme 1. H2020-EU.1.1. (EXCELLENT SCIENCE - European Research Council (ERC))
 Code Call ERC-2016-STG
 Funding Scheme ERC-STG
 Starting year 2017
 Duration (year-month-day) from 2017-02-01   to  2022-01-31

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    UNIVERSITAET INNSBRUCK AT (INNSBRUCK) coordinator 1˙425˙986.00
2    LUDWIG-MAXIMILIANS-UNIVERSITAET MUENCHEN DE (MUENCHEN) participant 70˙677.00

Map

 Project objective

Halogenated arenes and heteroarenes have become essential structural motifs of the pharmaceutical industry to create novel drugs against bacterial infections and cancer, and constitute highly valuable functional units in chemistry. Current methods for the installation of carbon-halogen bonds lack efficiency, selectivity, and practicability within the complex molecular setting of drug development processes. These restrictions prevent many potential drugs from being synthesized in a time- and cost-efficient manner. In this project, I aim to address these challenges by engineering a highly elaborated synthetic toolbox that is equipped with novel transformations of unprecedented efficiency, selectivity and practicability. I will apply these transformations to the construction of novel antibiotics against resistant strains and more efficient chemotherapeutics to combat cancer. The first objective is to establish innovative transformations that enable for the first time an efficient access to halogenated arenes. I will accomplish this goal by developing novel ring-expansion reactions and apply them to the first synthesis of the antibiotic salimabromide in order to address the acute problem of antibiotic resistance. Within the second part of this project, I will extend this unique synthetic platform to heteroarenes and establish a groundbreaking method based on carbon-fluorine bond activation. This will represent the first broadly applicable strategy to produce novel fluorinated heteroarene based anti-cancer drugs with unparalleled precision, efficiency and selectivity. Taken together, the realization of these strategies, all of which are unprecedented, provides for the first time a solution for the limitations associated with current methods. With my expertise in synthetic chemistry, which I have gained from my achievements in natural product synthesis, and an outstanding publication record in this research field, I am confident to accomplish these ambitious goals.

 Publications

year authors and title journal last update
List of publications.
2019 Matthias Schmid, Adriana S. Grossmann, Peter Mayer, Thomas Müller, Thomas Magauer
Ring-expansion approaches for the total synthesis of salimabromide
published pages: 3195-3215, ISSN: 0040-4020, DOI: 10.1016/j.tet.2019.03.010 		Tetrahedron 75/24 2019-08-29
2017 Raphael Wildermuth, Klaus Speck, Franz-Lucas Haut, Peter Mayer, Bianka Karge, Mark Brönstrup, Thomas Magauer
A modular synthesis of tetracyclic meroterpenoid antibiotics
published pages: , ISSN: 2041-1723, DOI: 10.1038/s41467-017-02061-7 		Nature Communications 8/1 2019-06-13
2018 Johannes Feierfeil, Thomas Magauer
De Novo Synthesis of Benzannelated Heterocycles
published pages: 1455-1458, ISSN: 0947-6539, DOI: 10.1002/chem.201705662 		Chemistry - A European Journal 24/6 2019-06-13
2018 Matthias Schmid, Adriana S. Grossmann, Klaus Wurst, Thomas Magauer
Total Synthesis of Salimabromide: A Tetracyclic Polyketide from a Marine Myxobacterium
published pages: , ISSN: 0002-7863, DOI: 10.1021/jacs.8b06228 		Journal of the American Chemical Society 2019-06-13
2017 Raphael Ernst Wildermuth, Tatjana Huber, Thomas Magauer
9-Membered Carbocycles: Strategies and Tactics for their Synthesis
published pages: , ISSN: 0947-6539, DOI: 10.1002/chem.201705919 		Chemistry - A European Journal 2019-06-13

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The information about "HALODRUGSYN" are provided by the European Opendata Portal: CORDIS opendata.

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