New gold catalysts for enantioselective cyclization reactions

用于对映选择性环化反应的新型金催化剂

• 批准号: 413882120
• 负责人: Dr. Dagmar Scharnagel
• 金额: --
• 依托单位: Institut Català dInvestigació Quimica (ICIQ)
• 依托单位国家: 德国
• 项目类别: Research Fellowships
• 财政年份: 2018
• 资助国家: 德国
• 起止时间: 2017-12-31 至 2018-12-31
• 项目状态: 已结题
• 来源: https://gepris.dfg.de/gepris/projekt/413882120?language=en
• 关键词: New; gold; catalysts; enantioselective; cyclization

The efficient and stereoselective construction of complex molecular scaffolds is a major challenge for the synthesis of complex natural products and drug molecules. Gold catalysis proved to be especially suited for this task. Numerous chiral ligands have been developed to date that deliver the products of various enantioselective carbocyclization reactions with excellent enantioselectivity. Nevertheless, the substrate scope for which high optical purities can be achieved is often limited which restricts the application to the synthesis of target molecules.The objective of this project is the design of novel chiral ligands based on a biaryl phosphine framework. This architecture accounts for the unique linear coordination geometry in Au(I) complexes as it allows to position the chiral information distant from the metal binding phosphine but in close proximity to the site of reaction. In addition, the steric and electronic properties can be adjusted by several variable residues at the chiral ligand. The corresponding gold complexes will be evaluated in cyclization reactions and ultimately be used for the assembly of valuable scaffolds.

复杂分子支架的高效立体选择性构建是复杂天然产物和药物分子合成的主要挑战。金催化剂被证明特别适合这项任务。迄今为止，已经开发了许多手性配体，它们以优异的对映选择性提供各种对映选择性碳环化反应的产物。然而，由于能够实现高光学纯度的底物范围有限，限制了其在目标分子合成中的应用。本课题的目标是设计基于联芳基膦骨架的新型手性配体。这种结构解释了Au（I）络合物中独特的线性配位几何结构，因为它允许将手性信息定位在远离金属结合膦但靠近反应位点的位置。此外，手性配体上的几个可变残基可以调节其空间和电子性质。相应的金配合物将在环化反应中进行评估，并最终用于组装有价值的支架。