Difluoroenol phosphinates as difluoroenolate surrogates: synthesis and applications in defluorination and deoxygenative coupling
We report defluorinative and deoxygenative functionalization reactions of trifluoromethyl ketones mediated by the phospha-Brook rearrangement, offering a streamlined approach to selectively modifying fluorinated compounds. Trifluoromethyl ketones react with phosphine oxides to undergo a phospha-Brook rearrangement followed by β-fluoride elimination, providing difluoromethyl ketones in good yields. By tuning the reaction conditions, we achieved the selective one-pot synthesis of monofluoromethyl ketones and methyl ketones, demonstrating the method's versatility across a range of fluorine-containing derivatives. Furthermore, we successfully demonstrated a range of deoxygenative transformations of key intermediates, such as difluoroenol phosphinates, showcasing their potential as building blocks for diverse functionalizations. These findings not only expand the synthetic toolbox for fluorine-containing molecules but also highlight the utility of phosphinate intermediates in developing novel reaction pathways.
Authors
- Junichiro Yamaguchi (ORCID: https://orcid.org/0000-0002-3896-5882)
- Miki B. Kurosawa (ORCID: https://orcid.org/0000-0002-8995-5377)
- Hiroki Tanaka (ORCID: https://orcid.org/0000-0002-7404-3527)
- Shuhei Shimoyama (ORCID: https://orcid.org/0000-0002-3896-5882)
Institutions
- Waseda University (JP)
Publication Details
- Journal
- Chemical Science
- Published
- 2025-01-01
- DOI
- https://doi.org/10.1039/d5sc03915k
- Citations
- 3
- Primary Topic
- Fluorine in Organic Chemistry
- Type
- article
- Field-Weighted Citation Impact
- 2.37
Funders
- Waseda University
- Japan Society for the Promotion of Science
- Core Research for Evolutional Science and Technology