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Enantioselective Copper(I)-Catalyzed Borylative Aldol Cyclizations of Enone Diones


  • We thank the EPSRC for financial support and for a Leadership Fellowship (to H.W.L.). We thank Darryl W. Low (University of Edinburgh) for assistance in the preparation of substrates, and Gary S. Nichol (University of Edinburgh) for assistance with X-ray crystallography. Solvias AG and AllyChem are gratefully acknowledged for kind donations of chiral ligands and B2(pin)2, respectively. We thank the EPSRC National Mass Spectrometry Service Centre for providing high-resolution mass spectra.


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Piña colato? In the presence of a chiral CuI/bisphosphine complex and B2(pin)2, enone diones undergo diastereo- and enantioselective desymmetrization to deliver highly functionalized bicyclic products. The products can be used as substrates in additional transformations. pin=pinacolato, Cy=cyclohexyl.