Direct difluoromethylation of heterocycles using difluoroacetic acid

Activity: Talk or presentation typesLecture and oral contribution

John Nielsen - Speaker

  • Natural Products and Peptides
Oral presentation at the C-H Activation Session entitled "Direct difluoromethylation of heterocycles using difluoroacetic acid" (ORGN 560).
Here, I presented our discovery of an innate, technically simple procedure for direct C-H difluoromethylation of heteroaromatic compounds using off-the-shelf difluoroacetic acid as the difluoromethylating agent in the presence of silver nitrate and potassium persulfate as the preferred oxidant. The reaction is tunable as bi-difluoromethylated products can be obtained by controlling the reaction temperature and running the reaction under more forceful conditions. Herein, we wish to report our detailed investigations, mechanistical studies and the scope and limitations of this novel reaction as well as unfold and deploy this methodology for preparation of tool compounds for chemical biology and provide access to this hitherto untapped substituent in drug discovery.
22 Aug 2018

Event (Conference)

Title256th National Meeting and Exposition of the American-Chemical-Society (ACS) - Nanoscience, Nanotechnology and Beyond
Date19/08/201823/08/2018
LocationBoston, MA
Country/TerritoryUnited States

    Research areas

  • difluoromethylation, difluoroacetic acid, Minisci reaction, heterocyclic chemistry, drug discovery

ID: 209707440