Enantioselective β-Arylation of Ketones Enabled by Lithiation/Borylation/1,4-Addition Sequence Under Flow Conditions


  • W.S. and S.L.B. thank Novartis International AG for funding. The Varian NMR instrument used was supported by the National Institutes of Health (Grant No. CHE 9808061). We thank Dr. Meredeth A. McGowan and Dr. Christine Nguyen for assistance with the preparation of this manuscript.


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The first multistep asymmetric catalysis in flow has been realized using a lithiation/borylation/rhodium-catalyzed 1,4-addition sequence. The three-step sequence starts from readily available and inexpensive aryl bromides, affording β-arylated ketones in good yields with high levels of enantioselectivity.