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

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.

Field of science

  • /medical and health sciences/basic medicine/pharmacology and pharmacy/drug resistance/antibiotic resistance
  • /natural sciences/chemical sciences/organic chemistry/hydrocarbons
  • /medical and health sciences/clinical medicine/cancer
  • /natural sciences/chemical sciences/inorganic chemistry/inorganic compounds

Call for proposal

ERC-2016-STG
See other projects for this call

Funding Scheme

ERC-STG - Starting Grant

Host institution

UNIVERSITAET INNSBRUCK
Address
Innrain 52
6020 Innsbruck
Austria
Activity type
Higher or Secondary Education Establishments
EU contribution
€ 1 425 986,80

Beneficiaries (2)

UNIVERSITAET INNSBRUCK
Austria
EU contribution
€ 1 425 986,80
Address
Innrain 52
6020 Innsbruck
Activity type
Higher or Secondary Education Establishments
LUDWIG-MAXIMILIANS-UNIVERSITAET MUENCHEN

Participation ended

Germany
EU contribution
€ 70 677,50
Address
Geschwister Scholl Platz 1
80539 Muenchen
Activity type
Higher or Secondary Education Establishments