Contribution of Organofluorine Compounds to Pharmaceuticals
Top Cited Papers
Open Access
- 22 April 2020
- journal article
- review article
- Published by American Chemical Society (ACS) in ACS Omega
- Vol. 5 (19), 10633-10640
- https://doi.org/10.1021/acsomega.0c00830
Abstract
Inspired by the success of fluorinated corticosteroids in the 1950s and fluoroquinolones in the 1980s, fluorine-containing pharmaceuticals, which are also known as fluoro-pharmaceuticals, have been attracting attention for more than half of a century. Presently, about 20% of the commercial pharmaceuticals are fluoro-pharmaceuticals. In this mini-review, we analyze the prevalence of fluoro-pharmaceuticals in the market and categorize them into several groups based on the chemotype of the fluoro-functional groups, their therapeutic purpose, and the presence of heterocycles and/or chirality to highlight the structural motifs, patterns, and promising trends in fluorine-based drug design. Our database contains 340 fluoro-pharmaceuticals, from the first fluoro-pharmaceutical, Florinef, to the latest fluoro-pharmaceuticals registered in 2019 and drugs that have been withdrawn. The names and chemical structures of all the 340 fluorinated drugs discussed are provided in the Supporting Information.Funding Information
- Japan Society for the Promotion of Science (JP 18H02553, JP 18H04401)
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