The Many Roles for Fluorine in Medicinal Chemistry

Journal of Medicinal Chemistry
2008.0

Abstract

Drug candidates with one or more fluorines have become commonplace. The special nature of fluorine imparts a variety of properties to certain medicines, including enhanced binding interactions, metabolic stability, changes in physical properties, and selective reactivities. Advances in fluorine chemistry have presented to the synthetic chemist a wide variety of reagents for the selective introduction of fluorine or fluoroalkyl groups into specific locations in their target molecules. This Perspective will try to provide to the practicing medicinal chemist a guide to some of the effects that the introduction of fluorine can have on potential drug candidates, including recent examples of successful strategies along with a list of leading references to synthetic transformations that may be useful.

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