Molecular Complexity via Enantioselective Palladium Catalysed C-N Bond Formations

该项目涉及根据最近在布里斯托开发的方法开发新的氮杂-赫克环化和级联。该项目分为三个部分：1。钯催化氮杂Heck环化反应合成吡咯烷和哌啶2.对映体选择性Pd催化的氮杂-Heck染料。通过N-O氧化加成实现的新级联C-N键形成过程：该计划专注于开发对药物化学具有潜在广泛用途的新型不对称C-N键形成过程。提供一个通用的对映选择性氮杂Heck协议将解决有机合成中未满足的挑战，并将具有很高的影响。该计划是由重要的初步成果支撑;因此，在博士项目可以取得重大进展。该计划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领域。

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.