Brief Communication abstract
Nature Chemical Biology 5, 26 - 28 (2008)
Published online: 16 November 2008 | doi:10.1038/nchembio.128
Chemo-enzymatic fluorination of unactivated organic compounds
Andrea Rentmeister1, Frances H Arnold1 & Rudi Fasan1,2
Fluorination has gained an increasingly important role in drug discovery and development. Here we describe a versatile strategy that combines cytochrome P450–catalyzed oxygenation with deoxofluorination to achieve mono- and polyfluorination of nonreactive sites in a variety of organic scaffolds. This procedure was applied for the rapid identification of fluorinated drug derivatives with enhanced membrane permeability.
- Department of Chemistry and Chemical Engineering, California Institute of Technology 210-41, 1200 East California Boulevard, Pasadena, California 91125, USA.
- Present address: Department of Chemistry, University of Rochester, Hutchison Hall, RC Box 270216, Rochester, New York 14627, USA.
Correspondence to: Rudi Fasan1,2 e-mail: fasan@chem.rochester.edu
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