Contribution of Organofluorine Compounds to Pharmaceuticals

By M. Inoue, Yuji Sumii, N. Shibata. ACS Omega, 2020

1,216 citations recorded by the source corpus.

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first fluoro-pharmaceutical, Florinef, to the latest fluoro-pharmaceuticals registered in 2019 and drugs that have been withdrawn.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.

Subfields: Organic Chemistry, Pharmaceutical Science

View Paper: https://www.semanticscholar.org/paper/d2f777e9375d53d2baa4cf6c521e65f1d6a29168

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In Organic Chemistry

  1. Y. Ogawa
  2. Osamu Kobayashi
  3. K. Hirai
  4. Etsuko Tokunaga
  5. N. Shibata

In Pharmaceutical Science

  1. Y. Ogawa
  2. Osamu Kobayashi
  3. K. Hirai
  4. Etsuko Tokunaga
  5. N. Shibata

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