4.6 Article

Enantioselective synthesis of 4-substituted tetrahydroisoquinolines via palladium-catalyzed intramolecular Friedel-Crafts type allylic alkylation of phenols

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ORGANIC & BIOMOLECULAR CHEMISTRY
卷 13, 期 10, 页码 3086-3092

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c4ob02574a

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资金

  1. National Basic Research Program of China (973 Program) [2015CB856600]
  2. National Natural Science Foundation of China [21272253, 21332009, 21421091]

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Palladium-catalyzed asymmetric intramolecular Friedel-Crafts type allylic alkylation reaction of phenols was developed under mild conditions. In the presence of Pd-2(dba)(3) with (1R,2R)-DACH-phenyl Trost ligand (L2) in toluene at 50 degrees C, the reaction provides various C4 substituted tetrahydroisoquinolines with moderate to excellent yields, regioselectivity and enantioselectivity.

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