Skeletal editing has emerged as an appealing strategy for scaffold-hopping-based drug discovery, but the enantioselective single-atom skeletal editing of N-heteroarenes is challenging. Now, using trifluoromethyl N-triftosylhydrazones as carbene precursors, the enantiodivergent dearomative skeletal editing of indoles and pyrroles has been achieved through asymmetric carbon-atom insertion.
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