7765-65-3Relevant academic research and scientific papers
[Bis-(trifluoroacetoxy)iodo]benzene-Mediated Oxidative Direct Amination C–N Bond Formation: Synthesis of 1H-Indazoles
Zhang, Zhiguo,Huang, Yuanyuan,Huang, Guoqing,Zhang, Guisheng,Liu, Qingfeng
, p. 2426 - 2433 (2017/07/24)
An efficient [bis-(trifluoroacetoxy)iodo]benzene (PIFA)-mediated oxidative C-N bond formation is developed for the synthesis of 1H-indazoles from readily available arylhydrazones. The reaction tolerates a wide range of functional groups and has broad scope of substrates. Moreover, this method is a relative green and reliable method for rapid preparation of substituted 1H-indazoles under mild conditions.
Pd- and Cu-catalyzed C-H arylation of indazoles
Hattori, Keika,Yamaguchi, Kazuya,Yamaguchi, Junichiro,Itami, Kenichiro
experimental part, p. 7605 - 7612 (2012/09/07)
The palladium- and copper-catalyzed C-H arylation reactions of 1H- and 2H-indazoles with haloarenes are described. A PdCl2/phen/Ag 2CO3/K3PO4 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.
