Bench‐Stable Electrophilic Reagents for the Direct Di‐ and Trifluoroethylthiolation of Indoles

Abstract

AbstractTwo saccharine‐based electrophilic reagents were developed for the direct introduction of SCH2CF3 and SCH2CF2H motifs via a C−S bond forming reaction. Their large‐scale preparation and reactivity performance has been carefully examined, enabling access to a series of indoles through open‐flask reactions. Sulfone and sulfoxide analogs (S(O)nCH2RF, n=1,2) are also accessible by sequential oxidation reactions.