Copper catalysed formation of C-X bonds

铜催化的乌尔曼缩合反应代表了一种尚未开发的替代方案，可以使用Buchwald-Hartwig钯化学来形成碳杂原子键。然而，该系统的效率和基板范围较差。在过去的十年里，乌尔曼缩合的一个重大创新是双齿配体的使用，双齿配体被认为可以稳定循环上的催化物质，促进氧化加成，防止亲核试剂的过度配位。这改善了反应条件，减少了催化负荷；尽管铜系统仍然落后于钯系统。该项目将发现新的铜配体系统利用n -杂环碳（NHCs），与第二个配位基团。一项全面的研究将涵盖新的配体设计和反应条件，以开发优化的系统，以获得药物发现中有价值的基序。

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.