Direct Fluoroacylation of Indole with Perfluoroalkyl Iodides.

Functionalization of perfluoroalkyl compounds has shown huge potential in synthetic chemistry and drug development. Herein, we report a one-pot tandem perfluoroalkylation-defluorination reaction of indole, perfluoroalkyl iodide, and water in the presence of Na2S2O4. A wide array of indole derivatives were efficiently accessed with good yields under mild reaction conditions. The reaction is believed to undergo perfluoroalkylation and follow the defluorination hydrolysis pathway. This study represents an alternative approach for defluorination functionalization.

Direct fluoroalkylthiolation of indoles with iodofluoroethane enabled by Na2S2O4.

In this paper, we report an efficient approach for the direct fluoroalkylthiolation of indoles with iodofluoroethane in the presence of Na2S2O4. In this work, we employed readily available iodofluoroethane and Na2S2O4 as fluoroalkylthiolation reagents, featuring mild conditions and a wide range of indole substrates. In addition, fluoroalkylthiolated 2,3'-biindole derivatives can also be prepared by this method.