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Method demonstrates the formation of trifluoromethylindolines from anilines, suggesting new pathways for synthesizing complex molecules.
Rh(III)-catalyzed C-H bond activation and annulation of N-pyrimidyl-substituted anilines with CF3-imidoyl sulfoxonium ylides (TFISYs) have been disclosed, affording a variety of 2-trifluoromethylindolines that contain a quaternary carbon center. A cascade C-H imidoylmethylation, tautomerization, and intramolecular nucleophilic addition sequence is involved in the transformation. The reaction could be scaled up to 2 mmol. The protocol provides facile and straightforward access to biologically important indoline scaffolds with a trifluoromethyl and an amino functionality.
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Li et al. (2025) studied this question.
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