4.7 Article

Asymmetric synthesis of CF3- and indole-containing tetrahydro-β-carbolines via chiral spirocyclic phosphoric acid-catalyzed aza-Friedel-Crafts reaction

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ORGANIC CHEMISTRY FRONTIERS
卷 4, 期 7, 页码 1407-1410

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c7qo00229g

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资金

  1. National Natural Science Foundation of China [21572200]
  2. Fundamental Research Funds for the Central Universities

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An enantioselective aza-Friedel-Crafts alkylation reaction of indoles with 1-trifluoromethyl-3,4-dihydro-beta-carbolines catalyzed by a chiral spirocyclic phosphoric acid has been realized. This methodology provides a facile route to 1-trifluoromethyl-1-indole-substituted tetrahydro-beta-carbolines featuring a CF(3)(-)containing quaternary stereocenter in considerable yields and good enantioselectivities.

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