酰胺键骨架构建的手性催化剂及其催化的不对称串联环化反应研究

本研究项目围绕不对称催化的效率和选择性核心问题，以多变的酰胺键为骨架构建一系列新型的手性金属络合物催化剂、金属－有机双功能催化剂和有机分子双功能催化剂；依据手性配体-金属-底物或手性有机分子催化剂-底物之间的匹配关系，发展与新型手性催化剂相匹配的两组分或多组分的不对称串联环化反应或协同环化反应体系，如Michael-Michael环化、Michael-Aldol环化、Povarov环化、环加成反应、杂-Diels-Alder反应等等，合成相应的光学活性的、具有多立体手性中心的环己酮、吡咯、吡唑、四氢吡啶、四氢吡喃酮、喹啉、螺环羟吲哚等碳环或杂环化合物及其衍生物；在手性合成的基础上，探索和认识手性催化中手性诱导、传递和放大的科学规律，并对所合成的光学活性的碳环、杂环、螺环、并环、桥环化合物进行细胞活性和药理活性测试，为我国手性医药、农药和手性功能材料等方面的发展提供科学基础和技术支撑。

Focused on catalytic asymmetric core issues of efficiency and selectivity, a series of novel chiral metal complex catalysts, the metal-organic bifunctional catalysts and the organic molecules bifunctional catalysts will be designed and synthesized in this research project. According to the matching relationship between chiral ligand, metal and substrate or chiral organic molecule and substrate, asymmetric tandem cyclization reactions and concerted cyclization reactions, such as cascade Michael-Michael cyclization, tandem Michael-Aldol cyclization, Povarov cyclization, cycloaddition reaction, hetereo-Diels-Alder reaction etc., will be carefully selected and developed in order to furnish the corresponding optically avtive multistereogenic cyclohexanones, pyrroles, pyrazolidine, tetrahydropyridines, tetrahydropyran ketones, quinolines, spirocyclic oxindoles with excellent yields, enantioselectivities and diastereoselectivities. On the basis of synthesis of those potentially biological and pharmacological active carbocyclic, heterocyclic, spirocyclic, and the bridged ring compounds, it is another important task that exploring and understanding the scientific regulation of chiral induction, transmission and amplification in this research project. Finally, the biological and pharmacological activity will be preliminaryly evaluated for the resulting optically active cyclic compounds. The research contents of this research project will provide scientific methodology and technical support for the synthesis of optically active compounds, and further promote the development of chiral drugs, chiral pesticides and chiral functional materials in our country.