Synthesis of 2-CF3-indoles or 2-CF3-indolin-3-ones via anaerobic or aerobic reactions of N-phenylpyridin-2-amines with TFISYs.

Presented herein is a condition-controlled selective synthesis of 2-CF3-indoles or 2-CF3-indolin-3-ones based on the anaerobic or aerobic reaction of N-phenylpyridin-2-amines with trifluoromethyl imidoyl sulfoxonium ylides (TFISYs). This work not only discloses a novel reaction mode of TFISYs, but also provides a robust protocol for the effective functionalization of aniline derivatives leading to the concise and selective assembly of indole-related scaffolds bearing a pharmaceutically privileged CF3 unit.