4.7 Article

Palladium-catalyzed direct C-2 arylation of indoles with potassium aryltrifluoroborate salts

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 73, Issue 18, Pages 7428-7431

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jo801371w

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Funding

  1. Zhejiang Provincial Natural Science Foundation of China [R407106]
  2. Natural Science Foundation of China [205710631]

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Mild conditions have been developed to achieve Pd(OAc)(2)-catalyzed regioselective cross-coupling between indoles and potassium aryltrifluoroarylborates in the presence of Cu(OAc)(2) in acetic acid at room temperature. A variety of potassium aryltrifluoroborates selectively undergo the direct arylation across indoles and afford 2-aryl indoles in moderate to good yields.

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