4.5 Article

Metal- and Base-Free Direct N-Arylation of Pyridazinones by Using Diaryliodonium Salts: An Anion Effect

Journal

ASIAN JOURNAL OF ORGANIC CHEMISTRY
Volume 7, Issue 8, Pages 1674-1680

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/ajoc.201800268

Keywords

anions; arylation; diaryliodonium salts; radical reactions

Funding

  1. National Nature Science Foundation of China [NSFC 21472213, 21772039]
  2. National Key Program [2016YFA0200302]
  3. Fundamental Research Funds for the Central Universities
  4. Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences

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An efficient N-arylation of pyridazinones with diaryliodonium salts has been developed without using base or metal catalysts. The reaction tolerated a variety of both diaryliodonium salts and pyridazinone derivatives with diverse functional groups. Furthermore, a drug candidate for treatment of neuropathic pain was synthesized with this procedure in good yield.

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