Diverse Synthesis of Chiral Trifluoromethylated Alkanes via Nickel‐Catalyzed Asymmetric Reductive Cross‐Coupling Fluoroalkylation

The trifluoromethyl group represents one of the most functional and widely used fluoroalkyl groups in drug design and screening, while the drug candidates containing chiral trifluoromethyl‐bearing carbons are still few due to the lack of efficient methods for the asymmetric introduction of trifluoromethyl group into organic molecules. Herein, we described a nickel‐catalyzed asymmetric trifluoroalkylation of aryl iodides, for the first time, by utilizing reductive cross‐coupling in enantioselective fluoroalkylation. This novel method has demonstrated high efficiency, mild conditions, and excellent functional group tolerance, especially for substrates containing diverse pharmaceutical and bioactive molecules moieties. This strategy provided an efficient and facile way for diversity‐oriented synthesis of chiral trifluoromethylated alkanes. We described a nickel‐catalyzed asymmetric trifluoroalkylation of aryl iodes, by demonstrating the first example of enantioselective reductive cross‐coupling fluoroalkylation with high efficiency, mild conditions, and excellent functional group tolerance, especially for diverse pharmaceutical and bioactive complex molecules. This strategy provided an efficient and facile way for diversity‐oriented synthesis of chiral trifluoromethylated alkanes.