Departamento de Química Orgánica I, Centro de Investigación y Estudios Avanzados "Lucio Lascaray"-Facultad de Farmacia, University of the Basque Country, UPV/EHU Paseo de la Universidad 7, 01006 Vitoria-Gasteiz, Spain.
Stratingh Institute for Chemistry, University of Groningen, 9747 AG Groningen, The Netherlands.
Molecules. 2021 May 27;26(11):3202. doi: 10.3390/molecules26113202.
Due to their structural similarity with natural α-amino acids, α-aminophosphonic acid derivatives are known biologically active molecules. In view of the relevance of tetrasubstituted carbons in nature and medicine and the strong dependence of the biological activity of chiral molecules into their absolute configuration, the synthesis of α-aminophosphonates bearing tetrasubstituted carbons in an asymmetric fashion has grown in interest in the past few decades. In the following lines, the existing literatures for the synthesis of optically active tetrasubstituted α-aminophosphonates are summarized, comprising diastereoselective and enantioselective approaches.
由于其与天然α-氨基酸的结构相似，α-氨基膦酸衍生物是已知的具有生物活性的分子。鉴于四取代碳在自然界和医学中的相关性以及手性分子的生物活性与其绝对构型的强烈依赖性，过去几十年中，不对称合成带有四取代碳的α-氨基膦酸酯的兴趣日益浓厚。在下面的几行中，总结了现有文献中关于光学活性的四取代α-氨基膦酸酯的合成方法，包括非对映选择性和对映选择性方法。
