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

与醇的 C-H 烷基化：使用醇作为亲电子试剂，通过碳阳离子促进氧化加成进行双催化 C-H 烷基化

• 批准号: 2605822
• 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: 2021
• 资助国家: 英国
• 起止时间: 2021 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2605822
• 关键词: Alkylation; Alcohols; Dual; Catalytic; using

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.

这项研究将开发使用醇作为烷基化试剂的钯催化的 C-H 键烷基化。 C-H 官能化在复杂分子的构建中带来了显着的优势，避免了预官能化。迄今为止，C-H 烷基化比其他 C-H 官能化工艺发展得还不够，并且通常依赖于有毒的烷基卤化物。在这里，将开发一种双催化系统，使用醇作为烷基化剂。这项工作将扩大目前有限的C-H烷基化反应范围，并避免对活化烷基卤化物的需求。反应开发（命中查找）和优化 (DOE) 将借助自动化（ROAR 中的 Freeslate 平台）进行，以快速确定反应空间范围。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合作，并可能包括进行实习的可能性。