J.Am.Chem.Soc.2017,139,9819～9822非编码光学活性的α,α-二取代α-氨基酸是有机合成和药物研发中一类非常重要的有机合成中间体,而对醛亚胺席夫碱进行直接不对称烯丙基化反应是制备非天然氨基酸的最有效和简单的方法之一.尽管该方法原料易得,操作简单,易于衍生,但由于拥挤的立体空间和前手性亲核试剂的立体选择性难以控制等因素限制了该反应的发展.此外,对多肽结构的后期修饰已经成为一种必要且灵活的方法,用于开发和研究新型的多肽药物.尽管过渡金属催化 J. Am. Chem. Soc. 2017, 139, 9819-9822 The non-coded optically active α, α-disubstituted α-amino acids are a very important class of organic synthesis intermediates in organic synthesis and drug discovery. Amine Schiff base direct asymmetric allylation is one of the most effective and simple methods for preparing unnatural amino acids.Although the raw materials are easy to obtain, easy to operate and easy to derivatize, due to the crowded three-dimensional space and front hand In addition, the post-modification of the polypeptide structure has become a necessary and flexible method for the development and research of novel peptide drugs.Although the transition metal catalytic