Synthesis of 2‐Phosphoryl‐3‐Monofluorovinylindoles under Catalyst‐ and Additive‐Free Conditions

Abstract A synthetic approach for the synthesis 2‐phosphoryl‐3‐monofluorovinylindoles via cascade regioselective dehydrative phosphorylation/stereoselective defluorination of difluoromethylated 3‐indolylmethanols and H ‐phosphine oxides under catalyst‐ and additive‐free conditions is described. The reaction could be scaled‐up without the need for column chromatography purification. magnified image