环状磷酰胺(硫代磷酰胺)骨架结构广泛存在于许多具有生物活性的分子中。异硫氰酸二烷氧(硫)基膦酯用于构建环状磷酰胺(硫代磷酰胺)化合物的报道很少，尤其是将这类化合物用于不对称催化反应的研究，从未见报道。基于我们在异硫氰酸基(-NCS)取代的化合物在不对称合成方面的研究积累，将开展异硫氰酸二烷氧(硫)基膦酯参与的不对称催化串联反应的研究。通过反应底物及催化体系的设计，实现异硫氰酸二烷氧(硫)基膦酯参与的不对称aldol/cyclization、Mannich/cyclization、Michael/cyclization、[3+3]及[3+4]类型的串联反应，建立高效合成手性环状磷酰胺(硫代磷酰胺)类化合物的新方法，研究各因素对反应活性及立体选择性的影响，揭示其反应规律。此项目的开展对于丰富不对称催化方面的研究，以及为手性环状磷酰胺(硫代磷酰胺)类化合物在新药的开发及合成应用方面具有重要意义。

Cyclophosphonamide/Cyclothioxophosphonamide moieties are commonly occurring heterocyclic ring systems found in many pharmaceuticals and bioactive molecules. There are a few reports in the literature about the application of isothiocyanato dialkoxylphosphines for the construction of cyclophosphonamide compounds. However, so far there are no any reports on the study of isothiocyanato dialkoxylphosphines/dithiolphosphines for the asymmetric catalysis. Based on our many researches on the catalytic asymmetric reaction and isothiocyanato compounds for the asymmetric organic synthesis, in this project, we will carry out the studies on the application of isothiocyanato dialkoxylphosphines/dithiolphosphines in the catalytic asymmetric cascade reaction. We hope to develop several asymmetric catalytic systems, including asymmetric aldol/cyclization, Mannich/cyclization, Michael/cyclization, formal [3+3], and formal [3+4] cascade reactions, by using isothiocyanato dialkoxylphosphines/dithiolphosphines with diverse reaction substrates. Meanwhile, we also will systemically study various influence factors on the reactivity, diastereo- and enantioselectivity, as well as disclose the possible reaction mechanism. The realization of this project will not only provide a viable approach for the construction of optically active structurally diverse cyclophosphonamide/cyclothioxophosphonamide compounds, and also offer a promising future in the library synthesis and new drug development.