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 SCF₃ and SCF₂H moieties. Herein, two saccharin-based electrophilic reagents have been disclosed for the incorporation of uncommon SCF₂CF₂H and SCF₂CF₃ motifs. Their reactivity performance, multigram-scale preparation, and divergent derivatization have been thoroughly investigated with a variety of nucleophiles, including natural products and pharmaceuticals.

中文翻译：

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用于直接掺入不常见 SCF2CF2H 和 SCF2CF3 基序的亲电试剂


氟烷基硫醚基团的引入引起了药物发现界的关注，因为它们赋予生物活性化合物特殊的理化和药代动力学特征，但这些基团通常仅限于标准 SCF ₃和 SCF ₂ H 部分。本文中，已经公开了两种基于糖精的亲电试剂用于掺入不常见的SCF ₂ CF ₂ H和SCF ₂ CF ₃基序。它们的反应性能、多克规模的制备和不同的衍生化已经用各种亲核试剂（包括天然产物和药物）进行了彻底研究。