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Application of the Pentafluorosulfanyl Group as a Bioisosteric Replacement.

08:00 EDT 7th August 2017 | BioPortfolio

Summary of "Application of the Pentafluorosulfanyl Group as a Bioisosteric Replacement."

The success of fluorinated molecules in drug design has led medicinal chemists to search for new fluorine-containing substituents. A major recently developed group is the pentafluorosulfanyl group. This group is stable under physiological conditions and displays unique physical and chemical properties. Currently, few synthetic methods exist that install the SF5 group, yet efforts to integrate this group into lead optimization continue unabated. Typically, the SF5 group has been used as a replacement for a trifluoromethyl, a tert-butyl, a halogen, or a nitro group. In this review, the use of the SF5 group as a bioisosteric replacement for each of these three functionalities will be compared and contrasted across different groups of biologically active molecules. The organization and presentation of these data are instructive to medicinal chemists considering to design synthetic strategies to access SF5 substituted molecules.

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This article was published in the following journal.

Name: ChemMedChem
ISSN: 1860-7187
Pages:

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Medical and Biotech [MESH] Definitions

Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)

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