299914-35-5

Upstream product

• 6146-52-7 5-nitroindole 
• 350-46-9 4-Fluoronitrobenzene 
• 32685-24-8 N-[4-(methylphenyl)sulfonyl]-5-nitro-1H-indole 
• 636-98-6 p-nitrobenzene iodide 

Relevant academic research and scientific papers

Synthesis of 1-aryl indoles via coupling reaction of indoles and aryl halides catalyzed by CuI/metformin

Ullmann-type C-N coupling reaction has been developed for the synthesis of 1-aryl indole derivatives by indoles and aryl halides in the presence of CuI/metformin (CuI/Met) in DMF. This method is very easy, rapid, and high yielding reaction for the synthesis of 1-aryl indoles. In particular, the metformin, which is used as ligand, is inexpensive and nontoxic that is considered to be relatively environmentally benign.

One-Pot N-Arylation of indoles directly from N-arylsulfonylindoles via consecutive deprotection and SnAr reactions with activated aryl halides

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

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

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.

Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles

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.

Method for arylating aza-heterocycles with activated aromatic compounds in the presence of caesium carbonate

The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.