近年来具有碳氮轴手性化合物的不对称合成受到极大的关注，但目前仍然缺乏实用的不对称合成方法来实现具有碳氮轴手性的天然产物和药物分子的高效合成。本项目拟通过设计新型手性噁唑啉配体和催化模式来发展一个高效普适的不对称Chan-Evans-Lam碳氮偶联反应方法学。利用该不对称偶联反应合成一系列具有潜在应用价值的碳氮轴手性化合物。探索该不对称碳氮偶联反应在天然产物和药物分子合成中的应用，最终实现具有合成难度的碳氮轴手性天然产物murrastifoline F、marinopyrrole A、ancistrocladinium A和xiamycin dimer的高效不对称全合成，以及轴手性药物telenzepine和CP-465022的简洁合成。与此同时，本项目将详细研究不对称Chan-Evans-Lam偶联反应的机理，阐明配体结构对偶联反应活性和对映选择性的影响。

The asymmetric synthesis of C-N axially chiral compounds has attracted significant attention. However, practical synthetic methods are still lacking and desirable for the synthesis of C-N axially chiral natural products and drug molecules. To address this challenge, an efficient and general asymmetric Chan-Evans-Lam C-N cross-coupling protocol will be developed in this programme through rational design of a series of chiral oxazoline ligands and catalysis mode. By using this coupling method, a wide range of valuable molecules with C-N axial chirality will be synthesized. The asymmetric cross-coupling will be applied to the synthesis of C-N axially chiral natural products including murrastifoline F, marinopyrrole A, ancistrocladinium A, and xiamycin dimer, as well as drug molecules, such as telenzepine and CP-465022. Meanwhile, the mechanism of the current Chan-Evans-Lam coupling will be investigate in order to illuminate the role of chiral ligands in the coupling reaction and their influence on reactivity and enantioselectivity. This research will provide an indepth understanding of ligand-facilitated Chan-Evans-Lam cross-coupling.