4.6 Review

Recent Advances in Transition-Metal-Free Late-Stage C-H and N-H Arylation of Heteroarenes Using Diaryliodonium Salts

Journal

PHARMACEUTICALS
Volume 14, Issue 7, Pages -

Publisher

MDPI
DOI: 10.3390/ph14070661

Keywords

diaryliodonium salts; C-H arylation; N-arylation; heteroarenes; metal-free; late-stage functionalization; eco-friendly

Funding

  1. LABEX SynOrg [ANR-11-LABX-0029]
  2. Universite de Rouen-Normandie (UNIROUEN)

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This review highlights recent synthetic advances in the late-stage C(sp2)-N and C(sp2)-C(sp2) bond-forming reactions under metal-free conditions using diaryliodonium salts as arylating reagents, and discusses their applications in the synthesis of new arylated bioactive heterocyclic compounds.
Transition-metal-free direct arylation of C-H or N-H bonds is one of the key emerging methodologies that is currently attracting tremendous attention. Diaryliodonium salts serve as a stepping stone on the way to alternative environmentally friendly and straightforward pathways for the construction of C-C and C-heteroatom bonds. In this review, we emphasize the recent synthetic advances of late-stage C(sp2)-N and C(sp2)-C(sp2) bond-forming reactions under metal-free conditions using diaryliodonium salts as arylating reagent and its applications to the synthesis of new arylated bioactive heterocyclic compounds.

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