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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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 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.

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

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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