Recent advances in light-driven synthesis of complex trifluoromethylated aliphatic amines and derivatives

Trifluoromethylated aliphatic amines, particularly those with structurally complex architectures, have emerged as valuable motifs in drug discovery due to their unique capacity to enhance metabolic stability, membrane permeability, and affinity for biological targets. However, the selective and efficient synthesis of these compounds remains a significant challenge, limiting their broader incorporation into pharmaceutical agents. Recent advances in light-driven organic synthesis, employing mild and sustainable visible-light-mediated conditions, have enabled modular and practical strategies for constructing these privileged structures from simple, readily available starting materials. A variety of photoinduced reactions, photocatalytic methods, and metallaphotoredox-catalyzed transformations have been developed, facilitating the direct installation of trifluoromethyl (CF₃) groups and CF₃-containing synthons onto diverse aliphatic frameworks and amine precursors. This review presents a comprehensive overview of recent progress in the photoinduced synthesis of trifluoromethylated aliphatic amines and their derivatives, emphasizing key methodological innovations, representative pharmaceutical targets, and mechanistic insights, with the goal of guiding future efforts in the design and synthesis of fluorine-rich bioactive molecules.