Catalytic Asymmetric Construction of CF3-Substituted Chiral sp3 Carbon Centers

Due to the unique steric and electronic nature of the fluorine atom, organofluorine compounds have received significant attention in the fields of pharmaceuticals and agrochemicals. In particular, the CF3 group is frequently found in biologically active compounds. However, compared to aryl- and alkenyl-CF3-containing molecules, the construction of sp(3) carbon-based alkyl-CF3-containing molecules, particularly via catalytic enantioselective synthesis, remains a considerable challenge in spite of their high potential in medicinal applications. This short review focuses on recent advances in this research area, and the reported strategies are categorized according to reaction types and starting substrates. In addition, chiral catalysts, substrate scope, and reaction mechanisms are briefly summarized.

Automated summary

This review focuses on the importance of organofluorine compounds in pharmaceuticals and agrochemicals, with particular emphasis on the challenges and recent advances in the catalytic enantioselective synthesis of sp(3) carbon-based alkyl-CF3-containing molecules.