PerspectiveChemistry

A New Departure in Fluorination Chemistry

Science  25 Sep 2009:
Vol. 325, Issue 5948, pp. 1630-1631
DOI: 10.1126/science.1179671

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Summary

Medicinal chemists often consider fluorine substitution of aromatics as a strategy for lead optimization, because the introduction of fluorine helps to rapidly improve pharmacokinetic and toxicological properties (1). Moreover, “editing” a lead structure with fluorine substitution can improve binding efficacy and selectivity. Traditional methods such as halogen exchange or diazonium-based transformations usually require reaction conditions that are too harsh for many aromatic molecules. These considerations have fueled interest in methodologies that are tolerant to functional group diversity, enabling fluorination of aromatics late in a synthetic sequence. On page 1661 of this issue, Watson et al. (2) report a novel palladium-catalyzed reaction that can be used to fluorinate a wide range of aromatics.

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