Literature DB >> 30912952

Palladium Catalyzed Hydrodefluorination of Fluoro-(hetero)arenes.

Joseph J Gair1, Ronald L Grey1, Simon Giroux1, Michael A Brodney1.   

Abstract

Palladium catalyzed hydrodefluorination was developed for fine-tuning the properties of fluoro-(hetero)aromatic compounds. The robust reaction can be set up in air, requires only commercially available components, and tolerates a variety of heterocycles and functionalities relevant to drug discovery. Given the prevalence of fluorine incorporation around metabolic hotspots, the corresponding deuterodefluorination reaction may prove useful for converting fluorinated libraries to deuterated analogues to suppress the oxidative metabolism by kinetic isotope effects.

Entities:  

Year:  2019        PMID: 30912952     DOI: 10.1021/acs.orglett.9b00889

Source DB:  PubMed          Journal:  Org Lett        ISSN: 1523-7052            Impact factor:   6.005


  2 in total

1.  Isotopic Radiolabeling of the Antiretroviral Drug [18F]Dolutegravir for Pharmacokinetic PET Imaging.

Authors:  Marion Tisseraud; Sébastien Goutal; Thomas Bonasera; Maud Goislard; Delphine Desjardins; Roger Le Grand; Chris M Parry; Nicolas Tournier; Bertrand Kuhnast; Fabien Caillé
Journal:  Pharmaceuticals (Basel)       Date:  2022-05-10

2.  Catalyst-Free Hydrodefluorination of Perfluoroarenes with NaBH4.

Authors:  Timothy D Schoch; Mukulesh Mondal; Jimmie D Weaver
Journal:  Org Lett       Date:  2021-02-15       Impact factor: 6.005

  2 in total

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