Cu(II)-Catalyzed Three-Component Sila-Strecker Reaction.

α-Aminosilanes have garnered significant attention as privileged structural motifs owing to their profound applications in pharmaceutical research, synthetic methodology, and advanced materials. We report here a general three-component Sila-Strecker reaction that utilizes an air- and moisture-stable Cu(II) salt catalyst, a silylation reagent, and ubiquitous starting materials, including a variety of amines (aryl amines, sulfamides, and sulfinamides) and carbonyl compounds (aldehydes and ketones). Diverse synthetically useful and pharmaceutically relevant α-aminosilanes are synthesized in moderate to excellent yields. Preliminary mechanistic investigation indicated an imine intermediate, which formed with the promotion of Ti(OEt)4. Compared with previous attempts, the established method offers a step-economic, operationally simple, and broadly tolerant approach that proceeds to α-aminosilane synthesis under mild conditions. Moreover, this reaction has been applied to the late-stage functionalization of a variety of bioactive natural products.