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Chemo-enzymatic fluorination of unactivated organic compounds.

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.

SUBMITTER: Rentmeister A

PROVIDER: S-EPMC2713661 | biostudies-literature | 2009 Jan

REPOSITORIES: biostudies-literature

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Chemo-enzymatic fluorination of unactivated organic compounds.

Rentmeister Andrea A Arnold Frances H FH Fasan Rudi R

Nature chemical biology 20081116 1

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. ...[more]

PMID: 19011638

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