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

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

*この研究の対応する著者

研究成果: Article査読

61 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)7605-7612
ページ数8
ジャーナルTetrahedron
68
37
DOI
出版ステータスPublished - 2012 9 16
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 創薬
  • 有機化学

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