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Article Abstract
By fine-tuning the electronic and steric properties of the chiral ligands, chiral Cu(II) complex-catalyzed enantioselective Friedel-Crafts alkylation/lactonization of 1-naphthols and electron-rich phenols with trifluoropyruvates provided the desired products with up to 99% ee and up to 99% yield. The reactions were carried out on a gram scale with low catalyst loading. Especially, the optically pure GABA positive allosteric modulator ()-BHFF was prepared using this protocol.
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