Copper catalysed formation of C-X bonds

铜催化的Ullmann缩合反应是使用Buchwald-Hartwig钯化学来形成碳-杂原子键的一种不发达的替代方法。然而，该系统存在效率较低和衬底范围较小的问题。在过去的十年中，Ullmann缩合反应的一个主要创新是使用了双齿配体，这些配体被认为可以稳定循环中的催化物种，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负载量的减少；尽管铜体系仍然落后于钯的对应物。这个项目将发现利用N-杂环卡宾(NHCS)的新的铜配体体系，并有第二个协调小组。将进行一项涵盖新配体设计和反应条件的全面调查，以开发在药物发现中访问有价值的基序的优化系统。

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.