Journal
JOURNAL OF FLUORINE CHEMISTRY
Volume 131, Issue 2, Pages 140-158Publisher
ELSEVIER SCIENCE SA
DOI: 10.1016/j.jfluchem.2009.09.009
Keywords
Fluorination; Agrochemistry; Pharmaceutical chemistry; Ethers; Thioethers; Amines; Phosphines; Fluoromethyl; Difluoromethyl; Trifluoromethyl
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Funding
- CNRS
- Bayer CropScience
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Fluorine, the most electronegative element plays nowadays a key role in pharmaceutical, agrochemical and material sciences. About 20% of all pharmaceuticals and about 30% of agrochemicals under development or recently introduced on the market contain fluorine. However, when one examines the relevant structures more closely, one quickly recognizes a structural monotony. The same fluorine bearing aromatic or heterocyclic cores appear over and over again. The search for novel molecules having emergent fluorinated groups and the development of an efficient access toward them is a challenging task for industrial as well as academic laboratories. For example, the trifluoromethoxy group finds increased utility as a substituent in bioactives, but it is still perhaps the least well understood fluorine substituent in currency. The present review will give an updated overview on the synthesis of alpha-fluorinated ethers, thioethers, amines and phosphines. (C) 2009 Elsevier B.V. All rights reserved.
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