A method for the electrochemical diastereoselective oxytrifluoromethylation of indoles was developed for the eco-friendly synthesis of CF3-containing spirocyclic indolines. The cascade reaction comprised anodic oxidation to obtain CF3 radicals, the addition of radicals to indoles, and intramolecular spirocyclization. The reaction system without external chemical oxidants could easily be scaled up. Antiproliferation assays of these CF3-substituted spirocyclic indolines exhibited their promising activities and selectivities toward several types of cancer cells, including Huh-7, A549, and cisplatin-resistant cancer cells (A549/DDP).
