Fluorinated Compounds in Medicinal Chemistry: Recent Applications, Synthetic Advances and Matched-Pair Analyses

Title:Fluorinated Compounds in Medicinal Chemistry: Recent Applications, Synthetic Advances and Matched-Pair Analyses

Volume: 14 Issue: 7

Author(s): David Barnes-Seeman, Jeremy Beck and Clayton Springer

Affiliation:

Keywords: Difluoroalkyl, fluorine, matched-pairs analysis, metabolic stability, pentafluorosulfanyl, trifluoromethylcyclopropyl.

Abstract: 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 matchedpair analysis to identify some interesting effects on in vitro ADME properties of replacing H by F on certain moieties.

Cite this article as:

Barnes-Seeman David, Beck Jeremy and Springer Clayton, Fluorinated Compounds in Medicinal Chemistry: Recent Applications, Synthetic Advances and Matched-Pair Analyses, Current Topics in Medicinal Chemistry 2014; 14 (7) . https://dx.doi.org/10.2174/1568026614666140202204242