1045601-61-3Relevant academic research and scientific papers
Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles
Xu, Hui,Liu, Wu-Qing,Fan, Ling-Ling,Chen, Yang,Yang, Liu-Meng,Lv, Lei,Zheng, Yong-Tang
, p. 720 - 722 (2008)
Eight simple N-arylindoles were designed, synthesized and evaluated as human immunodeficiency virus (HIV)-1 integrase inhibitors in vitro for the first time. Among these compounds, 3b, 3e and 3g demonstrated significant anti-HIV-1 integrase activity. Especially 3b showed the highest anti-HIV-1 integrase activity with EC50 value of 7.88 μg/ml and TI value of 24.61. Meantime, some structure-activity relationships were also observed and will provide a new lead for design and discovery of more potent N-arylindoles as HIV-1 integrase inhibitors.
One-Pot N-Arylation of indoles directly from N-arylsulfonylindoles via consecutive deprotection and SnAr reactions with activated aryl halides
Xu, Hui,Fan, Ling-Ling
experimental part, p. 321 - 323 (2009/11/30)
An efficient one-pot step by step t-BuOK-mediated procedure for the synthesis of N-arylindoles has been developed in moderate to good yields. The protocol involves the consecutive deprotection of N-arylsulfonylindoles as latent indoles and subsequent SnAr
Microwave-assisted N-arylation of indoles via C(sp2)-N(sp 2) bond formation by aromatic nucleophilic substitution reactions
Xu, Hui,Fan, Ling-Ling
experimental part, p. 298 - 302 (2009/01/31)
Microwave-assisted nucleophilic aromatic substitution on aryl halides with different indoles is described. Moderate to good yields are obtained in short reaction time (25-40 min) when coupling indoles with fluoro- and chloro-substituted aryl halides under catalyst-free conditions.
Ultrasound-assisted N-arylation of indoles without any catalyst
Xu, Hui,Lv, Lei,Fan, Ling-Ling,He, Xiao-Qiang
experimental part, p. 249 - 256 (2011/04/17)
An efficient method for the ultrasound-assisted N-arylation of indoles with haloarenes in an air atmosphere mediated by Cs2CO3 without any catalyst is reported. N-arylindoles are obtained in moderate to good yields while indoles cross-coupling with activated aryl halides (X = F or Cl). The Japan Institute of Heterocyclic Chemistry.
