New Methods to Access Enantioenriched Heterobicyclic Scaffolds

科尔、林赛和葛兰素史克的这一合作项目将探索通过交叉偶联-臭解-还原胺化策略快速制备对映体富集型杂双环支架的新方法。近年来，这种极性的三维结构因其良好的物理性质和对化学空间未被探索的区域的占据而吸引了相当大的药学兴趣。这一科学的基础是科尔早期开发的镁介导的不对称去质子化方法。葛兰素史克将为应用新兴的新方法带来确定相关药物目标和理想的分子结构方面的专业知识，以及与高通量化学和信息学相关的关键知识和设施。最终，这个项目将提供快速制备高度取代的有机终端产品的方法，这些最终产品将具有挑战性(或需要更长的路线)，通过其他方式获取，并且可能代表新的药物支架。EPSRC的主要研究领域是催化，化学反应动力学和机理，以及合成有机化学。

This collaborative project between Kerr, Lindsay, and GSK will explore new methods towards the rapid preparation of enantioenriched heterobicyclic scaffolds via a cross coupling-ozonoloysis-reductive amination strategy. Such polar, three-dimensional structures have attracted considerable pharmaceutical interest in recent years, due to their favourable physical properties and occupation of underexplored regions of chemical space. The science is underpinned by Kerr's earlier development of magnesium-mediated methods for asymmetric deprotonation. GSK will bring expertise in identifying relevant pharmaceutical targets and desirable molecular architectures for application of emerging new methods, as well as key knowledge and facilities as related to high throughput chemistry and informatics. Ultimately, this project will deliver methods to rapidly prepare highly substituted organic end-products, which would be challenging (or require lengthier routes) to access via other means, and which could represent new drug scaffolds.The main EPSRC research areas addressed are Catalysis, Chemical Reaction Dynamics and Mechanism, and Synthetic Organic Chemistry.