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Aqueous Benzylic C-H Trifluoromethylation for Late-Stage Functionalization.
- Source :
-
Journal of the American Chemical Society [J Am Chem Soc] 2018 Oct 03; Vol. 140 (39), pp. 12378-12382. Date of Electronic Publication: 2018 Sep 24. - Publication Year :
- 2018
-
Abstract
- The installation of trifluoromethyl groups has become an essential step across a number of industries such as agrochemicals, drug discovery, and materials. Consequently, the rapid introduction of this critical functional group in a predictable fashion would benefit current practitioners in those fields. This communication describes a mild trifluoromethylation of benzylic C-H bonds with high selectivity for the least hindered hydrogen atom. The reaction provides monotrifluoromethylation and proceeds in an environmentally friendly acetone/water solvent system. The method can be used to install benzylic trifluoromethyl groups on highly functionalized drug molecules.
Details
- Language :
- English
- ISSN :
- 1520-5126
- Volume :
- 140
- Issue :
- 39
- Database :
- MEDLINE
- Journal :
- Journal of the American Chemical Society
- Publication Type :
- Academic Journal
- Accession number :
- 30247886
- Full Text :
- https://doi.org/10.1021/jacs.8b08547