C-H Alkylation with Alcohols: Dual Catalytic C-H Alkylation using Alcohols as Electrophiles by Carbocation Promoted Oxidative Addition

本研究将发展以醇为烷基化试剂的钯催化C-H键烷基化反应。C-H官能化在避免预官能化的复杂分子的构建中具有显著的优势。迄今为止，C-H烷基化比其他C-H官能化方法发展得更少，并且通常依赖于有毒的烷基卤化物。在此，将开发双催化体系以使用醇作为烷基化剂。这一工作将扩大目前有限的C-H烷基化反应的范围，并避免了对活化的烷基卤化物的要求。将在自动化（注重成果的年度报告中的Freeslate平台）的帮助下进行反应开发（命中发现）和优化（DOE），以迅速确定反应空间。然后将详细研究成功的反应，以获得进一步的见解。该项目由阿斯利康共同资助并与阿斯利康合作，并可能包括进行安置的可能性。

This research will develop the palladium-catalysed alkylation of C-H bonds using alcohols as the alkylating reagent. C-H functionalisation promises significant advantages in the construction of complex molecules avoiding pre-functionalisation. To date, C-H alkylation is less developed than other C-H functionalisation processes, and commonly relies on toxic alkyl halides. Here, a dual catalytic system will be developed to employ alcohols as alkylating agents. This work will expand the currently limited scope of C-H alkylation reactions, and avoid the requirement for activated alkyl halides. Reaction development (hit finding) and optimisation (DOE) will be performed with the aid of automation (Freeslate platforms in ROAR), to rapidly scope out the reaction space. Successful reactions will then be studied in detail for further insights. This project is co-funded by and in collaboration with AstraZeneca, and may include the possibility to undertake a placement.