轴手性联芳基结构普遍存在于具有生物活性的天然产物、药物分子和手性材料中。此外，它们还作为核心骨架构成了一系列重要的手性配体和催化剂并在不对称催化中得到广泛的应用。近年来，新兴的轴手性化学领域得到了较大的发展，但是高效、快速构建轴手性骨架的催化不对称合成方法还相对有限，一些优势结构的轴手性配体与催化剂的价格仍十分昂贵，极大的限制了进一步的开发应用。本项目的主要研究目标就是发展经济、环境友好及条件温和的不对称交叉偶联方法制备光学活性轴手性化合物，解决相当一部分重要轴手性分子的来源问题。其核心研究策略是通过吸电子取代基活化芳环，将不稳定负电荷中间体快速转化，在有机小分子催化剂的作用下通过不对称C-H官能化实现轴手性联芳基骨架的立体选择性构建。除本课题组已报道的偶氮基团外，高价碘、硝基、亚胺等都将被用作活化与导向基团进行实验测试，同时，我们期望底物的普适性及中间体的可塑造性会带来产物的多样性。

Optically active atropisomeric biaryl motif is widespread in various bioactive natural products, pharmaceuticals and chiral materials. They also constitute the core structures of a series of important ligands and catalysts which are widely used in asymmetric catalysis. Despite remarkable advance has been achieved in the recent years, universal and facile approaches to access the axially chiral scaffolds are still highly desirable. The lack of concise enantioselective cross-coupling mounts to unacceptably high production cost for their commercialization which in turn greatly impeded their applications in related research area. In this context, our program aims to partially solve the source of useful atropisomerically enriched molecules through pursuing cost-effective and environmental-benign synthetic routes. The central strategy of our proposal is the installation of electron-withdrawing group to activate the arene and the rapid conversion of the unstabilized negative charged intermediate. Aided by the organocatalyst, the asymmetric C-H functionalization could be realized under mild reaction conditions to give the atropisomers with excellent stereocontrol. Apart from the azo group developed by our group very recently, other activating and directing groups including hypervalent iodine, nitro as well as imine will be systematically investigated. It is expected that the wide substrate scope and the flexibility of the intermediates are conducive to construct structurally diversified atropisomeric biaryl library for further application exploration.