Molecular Complexity via Enantioselective Palladium Catalysed C-N Bond Formations

该项目涉及根据最近在布里斯托尔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.通过对映体选择性钯催化的氮杂环化反应合成吡咯烷和哌啶类化合物。对映体选择性Pd催化的氮杂-Heck级联。由N-O氧化加成实现的新的级联C-N键形成方法：该计划集中于开发新的不对称C-N键形成方法，这些方法在药物化学中具有潜在的广泛用途。提供一个通用的对映体选择性氮杂-海克协议将解决有机合成中一个尚未满足的挑战，并将产生很大的影响。该方案以重要的初步成果为基础；因此，博士项目可以取得重大进展。该课程将对学生进行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培训。

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.