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Electrophilic Reagents for the Direct Incorporation of Uncommon SCF(2)CF(2)H and SCF(2)CF(3) Motifs
[Image: see text] The introduction of fluoroalkylthioether groups has attracted the attention of the drug-discovery community given the special physicochemical and pharmacokinetic features they confer to bioactive compounds, yet these are often limited to standard SCF(3) and SCF(2)H moieties. Herein...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9400389/ https://www.ncbi.nlm.nih.gov/pubmed/35944166 http://dx.doi.org/10.1021/acs.joc.2c01038 |
Sumario: | [Image: see text] The introduction of fluoroalkylthioether groups has attracted the attention of the drug-discovery community given the special physicochemical and pharmacokinetic features they confer to bioactive compounds, yet these are often limited to standard SCF(3) and SCF(2)H moieties. Herein, two saccharin-based electrophilic reagents have been disclosed for the incorporation of uncommon SCF(2)CF(2)H and SCF(2)CF(3) motifs. Their reactivity performance, multigram-scale preparation, and divergent derivatization have been thoroughly investigated with a variety of nucleophiles, including natural products and pharmaceuticals. |
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