Thiocarbonyl‐Directed Rhodium‐Catalyzed C2‐Selective C─H Bond Activation and Cyclization of N , N ‐Dimethylthioamide Indoles With Alkynes

The thiocarbonyl‐directed rhodium‐catalyzed C2‐selective C─H bond activation and cyclization of N , N ‐dimethylthioamide indoles with alkynes have been proposed, resulting in the efficient production of a series of substituted pyrrolo[1,2‐ a ]indole‐3‐thiones. The synthetic potential and mechanism of this strategy have also been preliminarily investigated. This protocol possesses the following advantages: stable and easily available substrates, redox‐neutral and concise conditions, precise C2‐selective C─H functionalization of indoles, and cyclic products with the retention of thiocarbonyl.