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Nat Chem Biol. 2009 Jan;5(1):26-8. doi: 10.1038/nchembio.128. Epub 2008 Nov 16.

Chemo-enzymatic fluorination of unactivated organic compounds.

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1
Department of Chemistry and Chemical Engineering, California Institute of Technology 210-41, 1200 East California Boulevard, Pasadena, California 91125, USA.

Abstract

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.

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PMID:
19011638
PMCID:
PMC2713661
DOI:
10.1038/nchembio.128
[Indexed for MEDLINE]
Free PMC Article

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