γ-Aminobutyric acid is a major inhibitory neurotransmitter in the mammalian central nervous system that plays a substantial role in brain disorders. γ-Amino phosphonic acid is a unique surrogate of both natural and unnatural γ-amino acid. Because of their unique biological activity, γ-amino acid and γ-amino phosphonic acid derivatives have attracted considerable attention. However, an efficient and straightforward method for constructing chiral γ-substituted-γ-amino acid and γ-amino phosphonic acid derivatives remains a long-standing challenge. Herein, a highly efficient, versatile, and universal Cu-catalyzed asymmetric hydroamination of cinnamyl esters, cinnamyl phosphonates, and cinnamyl phosphine oxides is presented for accessing γ-amino acid and γ-amino phosphonic acid derivatives in good yields with high levels of enantiocontrol and regioselectivity.

γ-氨基丁酸是哺乳动物中枢神经系统中的主要抑制性神经递质，在脑部疾病中起重要作用。γ-氨基膦酸是天然和非天然γ-氨基酸的独特替代品。由于其独特的生物活性，γ-氨基酸和γ-氨基膦酸衍生物引起了相当多的关注。然而，构建手性γ-取代-γ-氨基酸和γ-氨基膦酸衍生物的有效且直接的方法仍然是一个长期存在的挑战。在此，一种高效、通用且通用的铜催化肉桂酯、肉桂膦酸酯、