4.7 Article

Facile synthesis of 1-aminoindoles via Rh(III)catalysed intramolecular three-component annulation

Journal

ORGANIC CHEMISTRY FRONTIERS
Volume 4, Issue 11, Pages 2179-2183

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c7qo00541e

Keywords

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Funding

  1. NSF of China [21572072, 21602064]
  2. Xiamen Southern Oceanographic Center [15PYY052SF01]
  3. Science and Technology Bureau of Xiamen City [3502Z20150054]

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The facile synthesis of various 1-aminoindoles from readily available aryl hydrazines, diazo compounds and ketones via rhodium catalysed C-H activation has been developed. The reaction was carried out under mild reaction conditions using hydrazone as a directing group, which was formed by the in situ condensation of hydrazines and ketones. This protocol exhibits a broad substrate scope and step economy, releasing N-2 and H2O as the byproducts, obviating the need for external oxidants and prefunctionalized substrates.

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