Since our lab’s first paper establishing a transient directing group strategy for asymmetric Heck-type hydroarylation went online in 2019, we’ve been hard at work trying to extend this approach to three-component 1,2-difunctionalization. At long last we’ve succeeded, and we are thrilled to report the fruits of our labor: a remarkably versatile 1,2-arylfluorination reaction that can form fully substituted C(sp³)–Ar and C(sp³)–F stereo centers in up to >99% ee. Pivotal to the success of the project was use of design of experiments (DoE) to facilitate rapid optimization of reaction conditions and reaction progress kinetic analysis (RPKA) to elucidate the reaction mechanism. Hats off to Zhonglin, Luke, Mingyu, Zi-Qi, Van, and Yang on the landmark achievement!

For a link, click here: https://chemrxiv.org/articles/preprint/A_Transient_Directing_Group_Strategy_Enables_Enantioselective_Multicomponent_Organofluorine_Synthesis/13537283