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!
The holiday paper flurry continues! ❄️⛄️🥶 This time it’s Team Nickel, who together with collaborators at Bristol Myers Squibb describe the use of Ni(COD)(DMFU) as a well-defined, all-in-one precatalyst for alkene diarylation. This lovely red free-flowing solid can be conveniently prepared in high yield from Ni(COD)2 and is indefinitely thermally stable as long as handled in an inert-atmosphere glovebox. Congrats to the Scripps team, Nana, Van, and Omar, as well as BMS team, Steve and Martin. Here’s to another great year to come in the Scripps–BMS collaboration!
For a link to the paper, click here: https://www.thieme-connect.com/products/ejournals/abstract/10.1055/a-1344-6040