Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 14, Issue 7, Pages 855-864Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026614666140202204242
Keywords
Difluoroalkyl; fluorine; matched-pairs analysis; metabolic stability; pentafluorosulfanyl; trifluoromethylcyclopropyl
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In recent years, several new fluorinated functional groups have been employed in medicinal chemistry. This review will highlight some recent developments in this area. We draw attention to useful synthetic advances for the installation of fluorine-containing groups. In addition, we examine the application of some fluorinated functional groups that have recently been gaining popularity in drug discovery. We use matched-pair analysis to assemble aggregate data on the impact on potency of one of these groups, pentafluorosulfanyl, as compared to trifluoromethyl. We further used matched-pair analysis to identify some interesting effects on in vitro ADME properties of replacing H by F on certain moieties.
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