Pd- and Cu-catalyzed C-H arylation of indazoles

Keika Hattori, Kazuya Yamaguchi, Junichiro Yamaguchi, Kenichiro Itami*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

73 Citations (Scopus)


The palladium- and copper-catalyzed C-H arylation reactions of 1H- and 2H-indazoles with haloarenes are described. A PdCl 2/phen/Ag 2CO 3/K 3PO 4 catalytic system is effective for the C-H arylation of 1H- and 2H-indazoles with haloarenes, whereas a less expensive CuI/phen/LiOt-Bu catalytic system is applicable to the C-H coupling of substituted 2H-indazoles and iodoarenes. The utility of newly developed catalyst was demonstrated in the rapid synthesis of YC-1 (an antitumor agent) and YD-3 (platelet anti-aggregating agent). These new reactions represent important direct functionalization tools of indazoles, well-known bioisosteres of pharmaceutically important indole core.

Original languageEnglish
Pages (from-to)7605-7612
Number of pages8
Issue number37
Publication statusPublished - 2012 Sept 16
Externally publishedYes


  • C-H arylation
  • Catalysis
  • Heterobiaryl
  • Indazole

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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