Towards an Atroposelective N-arylation of 2-pyridones by High-Throughput Integrated Methodological Synthetic Chemistry

通过高通量综合方法合成化学实现 2-吡啶酮的原子选择性 N-芳基化

• 批准号: 2751541
• 金额: --
• 依托单位: University of Cambridge
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2022
• 资助国家: 英国
• 起止时间: 2022 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2751541
• 关键词: Towards; Atroposelective; arylation; pyridones; Throughput

We have discovered and begun optimisation of a previously impossible C-N cross-coupling reaction capable of assembling sterically demanding N-aryl 2-pyridones. Through the integration of HTE into the methodological development process, we have been able to build a working reaction from the ground up in a relatively short period which already outperforms literature attempts at similar substrates, and if fully optimised will constitute an excellent tool for synthetic and medicinal chemists to use in accessing a previously troublesome class of molecules.The generality, atroposelectivity, and further applications of this new and powerful system are most exciting research prospects which we plan to explore with the continued use of an HTE-integrated approach.

我们已经发现并开始优化以前不可能发生的C-N交叉偶联反应，该反应能够组装空间要求极高的N-芳基2-吡啶酮。通过将HTE整合到方法学的开发过程中，我们已经能够在相对较短的时间内从基础上建立起工作反应，这已经超过了在类似底物上的文献尝试，如果完全优化，将成为合成和药物化学家访问以前麻烦的一类分子的极好工具。这种新的和强大的系统的通用性、可逆性和进一步的应用是最令人兴奋的研究前景，我们计划继续使用HTE-集成方法来探索。