New Catalytic Enantioselective Desymmetrisation Reactions

手性磷（V）化合物在农业化学和制药工业中具有高度重要性，因为许多成功的药物如Remdesivir和Sofosbuvir基于手性磷（V）基序。然而，迄今为止，只有少数报道的催化对映选择性方法可以用于产生具有高对映选择性和高纯度的新的此类化合物。这些方法只允许获得有限数量的特定类别的此类化合物。因此，一种新的方法，将打开这个相对未开发的化学空间将是非常有价值的。在这个项目中，我们将研究新的双功能手性催化剂，通过一种新的去对称化方法，有效地创造立体异构磷（V）物种具有高的对映选择性。考虑到在构建这些物种的骨架时可能实现的排列，将有望出现一种通用的和高度对映选择性的催化方法，该方法将提供对多个化合物类别的选择性访问。这些新方法的开发，并展示其在高生物和医学意义的分子合成中的应用将是这项工作的主要组成部分。该项目由阿斯利康福尔斯共同资助，属于EPSRC合成有机化学/催化研究领域。

Chiral phosphorous (V) compounds are of high importance in the agrochemical and pharmaceutical industries as many successful drugs such as Remdesivir and Sofosbuvir are based on chiral phosphorous (V) motifs. However, to date, there are only a few reported catalytic enantioselective methods which could be used to create new such compounds with high enantioselectivity and high purity. These methods allow access to only a limited number of specific classes of such compounds. Therefore, a new method that will unlock this relatively untapped chemical space will be highly valuable.During this project we will investigate new bifunctional chiral catalysts to efficiently create stereogenic phosphorus (V) species with high enantioselectivities through a novel desymmetrisation approach. Given the possible permutations that could be achieved when building the backbone of these species, a general and highly enantioselective catalytic method that will provide selective access to multiple compound classes, will hopefully arise. The development of these new methodologies, and demonstrating their application to synthesis of molecules of high biological and medicinal significance will be a major component of this work.This project which is co-funded be AstraZeneca falls within the EPSRC Synthetic Organic Chemistry/Catalysis research area.