Ligand-Accelerated Direct C−H Arylation of BINOL: A Rapid One-Step Synthesis of Racemic 3,3′-Diaryl BINOLs
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文摘
An ortho-selective rhodium-catalyzed direct C−H arylation of 1,1′-bi-2-naphthol (BINOL), to deliver the widely used but not easily available 3,3′-diaryl BINOL, has been developed. This highly efficient one-step synthetic approach is the shortest route to date and is greatly facilitated by the newly developed ligand system comprising tBu2PCl, Ph2-cod, and Cy3P⋅HBF4. In addition, the same procedure can facilitate the challenging syntheses of 3-bulkyaryl BINOLs in good to excellent yields.

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