轴手性联苯骨架伯叔二胺催化剂的设计、合成及在不对称反应中的应用研究

Chiral primary amine catalysis was paid more and more attention during the last few years. The excellent asymmetric induction of axial chiral ligand had been proved in the transition metal catalysis. In this project, the axially chirality are combined with primary amine catalysis to develop a novel kind of axially chiral primary amine organocatalyst. The main research contents include: (i) The use of kinetic resolution technology to prepare the axially chiral diphenyl-type diamine; (ii) Usage of chirality tranfer strategy to introduce axially chirality from central or axially chirality; (iii) The chiral primary amine library is expanded and the axial chiral primary amine catalysts are given more choice for asymmetric primary amine catalysis.(iV) The chiral qutertary carbon centre was induced by the primary amine catalysis. The relationship betwwen the activity and the structure of the catalysts would also been studied to uncover the mechanisms of the chirality transfer. This study would provide practical and theoretical support for the development of a new generation of highly efficient asymmetric catalysts.

手性伯胺催化是有机小分子催化中的一个研究热点。轴手性优异的手性诱导性在过渡金属催化中已得到证明。本项目拟将轴手性元素引入到伯胺催化中，发展新型轴手性伯胺催化剂。主要研究内容包括：（1）、利用手性拆分技术合成轴手性伯叔二胺催化剂；（2）、利用既有手性（中心手性和轴手性）诱导产生轴手性的策略合成新型轴手性联苯骨架伯胺催化剂；（3）、对伯叔二胺催化剂进行结构表征，拓展伯胺催化剂的种类，为不对称伯胺催化提供更多的选择；（4）将合成的轴手性伯胺催化剂应用到烯胺机理及亚胺机理催化的不对称反应中，构建手性季碳中心，研究取代基位阻效应和苯环电子效应对手性诱导的关系，揭示手性在分子间的传递机制，为开发新一代高效不对称合成催化剂提供实践和理论依据。

手性伯胺催化是有机小分子催化中的一个研究热点。轴手性优异的手性诱导性在过渡金属催化中已得到证明。本项目拟将轴手性元素引入到伯胺催化中，发展新型轴手性伯胺催化剂。主要研究内容包括:（1）、合成联苯型轴手性伯胺催化剂；（2）、对合成的催化剂进行结构表征；（3）拓展伯胺催化剂的种类，为不对称伯胺催化提供更多的选择；（4）探索联苯型轴手性伯胺催化剂的应用。