4.6 Article

Heterocyclic iodoniums as versatile synthons to approach diversified polycyclic heteroarenes

Journal

RSC ADVANCES
Volume 9, Issue 57, Pages 33170-33179

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c9ra07288h

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Funding

  1. National Natural Science Foundation of China [81672952, 81872440]
  2. Guangdong Science and Technology Program [2017A020215198, 2018A030310240]
  3. Guangzhou Science and Technology Program [201807010041]

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Polycyclic heteroarenes are important scaffolds in the construction of pharmaceuticals. We have previously developed a series of novel heterocyclic iodoniums. In our current work, these unique iodoniums were employed to construct various complex polycyclic heteroarenes with structural diversity via tandem dual arylations. As a result, indole, thiophene and triphenylene motifs were fused into these heterocycles with high molecular quality, which might provide promising fragments in drug discovery. Moreover, these heterocycles could be diversified at a late stage.

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