Copper catalysed formation of C-X bonds

铜催化C-X键的形成

• 批准号: 1955223
• 金额: --
• 依托单位: Imperial College London
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2017
• 资助国家: 英国
• 起止时间: 2017 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-1955223
• 关键词: Copper; catalysed; formation; bonds

Copper-catalysed Ullmann condensation reactions represent an under-developed alternative to the use of Buchwald-Hartwig palladium chemistry for the formation of carbon-heteroatom bonds. However, the systems suffer from poorer efficiency and substrate scope. In the last decade a major innovation in the Ullmann condensation is the use of bidentate ligands which are believed to stabilise on-cycle catalytic species, facilitating oxidative addition, and preventing over-coordination of the nucleophile. This has led to improved reaction conditions and reduced catalytic loading; though copper systems still lag behind their palladium counterpart.This project will discover new copper-ligand systems exploiting N-heterocyclic carbenes (NHCs), with a second coordinating group. A comprehensive investigation covering new ligand designs and reaction conditions will be carried out in order to develop optimised systems for accessing valuable motifs in drug discovery.

铜催化的Ullmann缩合反应代表了使用Buchwald-Hartwig钯化学形成碳-杂原子键的未开发的替代方案。然而，这些系统的效率和基底范围较差。在过去的十年中，Ullmann缩合的一个主要创新是使用双齿配体，其被认为稳定循环催化物质，促进氧化加成，并防止亲核试剂的过度配位。这导致了反应条件的改善和催化剂负载量的减少;尽管铜体系仍然落后于钯对应物。本项目将发现新的铜配体体系，利用具有第二配位基团的N-杂环卡宾（NHC）。一个全面的调查，包括新的配体设计和反应条件将进行，以开发优化的系统，在药物发现中访问有价值的图案。