Molecular Complexity via Enantioselective Palladium Catalysed C-N Bond Formations

通过对映选择性钯催化 C-N 键形成的分子复杂性

• 批准号: 1941711
• 金额: --
• 依托单位: University of Bristol
• 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-1941711
• 关键词: Molecular; Complexity; via; Enantioselective; Palladium

The project concerns the development of new aza-Heck cyclizations and cascades based upon methodology recently developed at Bristol. The project is split into three parts:1. The synthesis of pyrrolidines and piperidines via enantioselective Pd-catalysed aza-Heck cyclizations2. Enantioselective Pd-catalysed aza-Heck cascades.3. New cascade C-N bond forming processes enabled by N-O oxidative addition:The programme concentrates on the development of novel asymmetric C-N bond forming processes that are of potentially widespread utility to medicinal chemistry. The provision of a general enantioselective aza-Heck protocol will address an unmet challenge in organic synthesis, and will have high impact. The programme is underpinned by important preliminary results; as such, significant progress can be achieved in the PhD project. The programme will train the student in the areas of asymmetric organometallic catalysis, N heterocyclic chemistry and organometallic reaction mechanism.

该项目涉及基于布里斯托尔最近开发的方法开发新的aza-Heck循环和级联。本项目分为三个部分：1.设计方案；对映选择性pd催化aza-Heck环化合成吡咯烷和哌啶[j]。2 .对映选择性pd催化aza-Heck级联。由N-O氧化加成的新型级联C-N键形成过程：该计划专注于开发新的不对称C-N键形成过程，这些过程在药物化学中具有潜在的广泛用途。提供一种通用的对映选择性aza-Heck协议将解决有机合成中未满足的挑战，并将产生很高的影响。该方案以重要的初步结果为基础；因此，博士项目可以取得重大进展。该课程将培养学生在不对称有机金属催化、N杂环化学和有机金属反应机理方面的能力。

项目成果

Complex Polyheterocycles and the Stereochemical Reassignment of Pileamartine A via Aza-Heck Triggered Aryl C-H Functionalization Cascades.

• DOI: 10.1021/jacs.1c08615
• 发表时间: 2021-09-29
• 期刊: Journal of the American Chemical Society
• 影响因子: 15
• 作者: Jones BT;García-Cárceles J;Caiger L;Hazelden IR;Lewis RJ;Langer T;Bower JF
• 通讯作者: Bower JF