New Methods to Access Enantioenriched Heterobicyclic Scaffolds

获取对映体富集的杂双环支架的新方法

• 批准号: 2889459
• 金额: --
• 依托单位: University of Strathclyde
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2023
• 资助国家: 英国
• 起止时间: 2023 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2889459
• 关键词: New; Methods; Access; Enantioenriched; Heterobicyclic

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.

Kerr、Lindsay 和 GSK 之间的这个合作项目将探索通过交叉偶联-臭氧分解-还原胺化策略快速制备对映体富集的杂双环支架的新方法。近年来，这种极性三维结构因其良好的物理性质和占据化学空间中尚未开发的区域而引起了制药界的极大兴趣。该科学的基础是克尔早期开发的镁介导的不对称去质子化方法。葛兰素史克将带来在确定相关药物靶标和应用新兴新方法所需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，该项目将提供快速制备高度取代的有机最终产品的方法，这将具有挑战性（或需要更长的路线）通过其他方式获得，并且可能代表新的药物支架。 EPSRC 的主要研究领域是催化、化学反应动力学与机理、有机合成化学。