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

我们已经发现并开始优化以前不可能的C-N交叉偶联反应，能够组装空间要求高的N-芳基2-吡啶酮。通过将HTE整合到方法学开发过程中，我们已经能够在相对较短的时间内从头开始构建工作反应，该反应已经优于类似底物的文献尝试，并且如果完全优化，将构成合成和药物化学家用于访问先前麻烦的一类分子的极好工具。和进一步的应用，这个新的和强大的系统是最令人兴奋的研究前景，我们计划探索与继续使用的HTE集成的方法。

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.