Phosphonates and derivatives with an α-chiral center are of great importance and they are widely distributed in many natural products, pharmaceuticals, and agrochemicals with various bioactive features. Great effort has been made toward the development of efficient methods for their synthesis. In this short review, recent advances in the asymmetric catalytic synthesis of phosphonates with an α-chiral center are summarized, including asymmetric hydrogenation of α,β-unsaturated phosphonates, asymmetric addition of phosphonates to unsaturated electrophiles, and asymmetric addition of nucleophiles to α,β-unsaturated phosphonates. In addition, continuous development of enantioselective catalytic synthetic methods and the application of phosphonates and derivatives with α-chiral center are future prospects.

1 Introduction

2 Asymmetric Hydrogenation of α,β-Unsaturated Phosphonates

3 Asymmetric Addition of Phosphonates to Unsaturated Electrophiles

4 Asymmetric Addition of Nucleophiles to α,β-Unsaturated Phosphonates

5 Conclusion

具有α-手性中心的膦酸酯及其衍生物非常重要，它们广泛分布于许多具有多种生物活性特征的天然产物、药物和农用化学品中。已经为开发用于合成它们的有效方法做出了巨大努力。在这篇简短的综述中，总结了具有 α-手性中心的膦酸酯的不对称催化合成的最新进展，包括 α,β-不饱和膦酸酯的不对称氢化、膦酸酯对不饱和亲电子试剂的不对称加成，以及亲核试剂对 α 的不对称加成， β-不饱和膦酸盐。此外，对映选择性催化合成方法的不断发展以及具有α-手性中心的膦酸酯及其衍生物的应用是未来的前景。

1 简介

2 α,β-不饱和膦酸酯的不对称氢化

3 膦酸盐与不饱和亲电试剂的不对称加成

4 亲核试剂对α,β-不饱和膦酸盐的不对称加成

5 结论