METAL MEDIATED SCHIFF BASES FOR MEDICINAL AGENT SYNTHESIS

我们的研究旨在开发低成本和高效的不对称催化剂，用于药物合成的实际用途，例如合成对天然产物和/或伦理药物组分具有生物重要性的中间体。手性药物具有临床应用价值高、毒性低、低剂量低成本、对环境影响小等优点，被公认为未来的药物。本研究旨在解决手性药物化学发展中的重要问题。我们的方法包括手性配体的合理设计、合成和表征，以及通过掺入金属离子来开发配体的手性配合物。利用所开发的手性配合物作为催化剂，可以将廉价的前手性底物有机地转化为所需的手性化合物。该项目是我们开发手性席夫碱催化剂的逻辑延伸，该催化剂对构建生物活性药物具有重要意义。在手性配体中引入特殊的基序对配合物表现出高的对映选择性、高的反应活性和稳定性具有重要意义。本项目中提出的新手性催化剂将利用已发现的学科，使用最有效的空间效应基团及其位置，能够区分空间以实现高对映选择性。该催化剂被设计成具有Salen配体，该Salen配体具有“壁型”庞大基团以提供空间位阻，该空间位阻随着位置而优化。通过本研究，将建立微观结构与对映选择性之间的明确关系，并将预期用于实际应用的高效催化剂。

Our research is aimed to develop low-cost and highly efficient asymmetric catalysts for practical uses in pharmaceutical syntheses, e.g. synthesis of intermediates that are of biological importance for natural products and/or ethical drug components. Chiral medicines have been recognized as the medicines of the future of high clinical relevancy, low toxicity and cost-effectiveness of low dosage as well as minimization of environment impact. This research is to address important issues towards the chemistry development in chiral medicines. Our approach includes rational design, synthesis and characterization of chiral ligands as well as the development of chiral complexes from the ligands by incorporation of metal ions with. The organ transformation of inexpensive pro-chiral substrates into requisite chiral compounds will be achieved using the developed chiral complexes as catalysts. The project is a logic extension of our development of chiral Schiff bases catalysts for reactions important to the construction of bioactive medicinal agents. Special motifs induced into chiral ligands are important for complexes to exhibit high enantioselectivity, high reactivity and stability. New chiral catalysts proposed in this project will take advantage of discovered disciplines to use the most effective steric effect groups and their positions capable of differentiating space for high enantioselectivity. The catalysts are designed to have Salen ligands that possess "wall type" bulky groups to provide steric hindrance which is to be optimized with the position. Through this research, a clear correlation between microstructure and enantioselectivity will be established and efficient catalysts for practical application will be anticipated.