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

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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.