1026-22-8

Upstream product

• 221910-02-7 3-(2-aminophenyl)-1-(4-chlorophenyl)prop-2-yn-1-one 
• 24668-08-4 1-(4-chlorophenyl)-3-(2-nitrophenyl)prop-2-en-1-one 
• 823809-34-3 N-(2-aminobenzylidene)-4-methylaniline 
• 536-38-9 4-chlorobenzoylmethyl bromide 
• 18631-54-4 1-(4-Chloro-phenyl)-2-(dimethyl-λ⁴-sulfanylidene)-ethanone 
• 243844-35-1 N-[2-(chloromethyl)-phenyl]-4-methylbenzene-1-sulfonamide 
• 90312-02-0 N-(2-hydroxymethylphenyl)-4-methylbenzenesulfonamide 
• 529-23-7 o-aminobenzaldehyde 
• 6203-15-2 2,2,2-trifluoro-N-(2-formylphenyl)acetamide 
• 201230-82-2 carbon monoxide 
• 1679-18-1 4-Chlorophenylboronic acid 
• 167558-54-5 2-(2,2-dibromo-vinyl)-phenylamine 
• 231296-12-1 (1-phenylsulfonyl-1H-indol-2-yl)(4-chlorophenyl)methanone 
• 122-01-0 4-chloro-benzoyl chloride 

Relevant academic research and scientific papers

Synthesis of 2-Acylindoles via Ag- and Cu-Catalyzed anti-Michael Hydroamination of β-(2-Aminophenyl)-α,β-ynones: Experimental Results and DFT Calculations

β-(2-Aminophenyl)-α,β-ynones afforded 3-unsubstituted 2-acylindoles in good yields in the presence of 20 mol % AgOTf under (microwave) MW heating. The use CuOTf as a catalyst resulted in a similar reaction outcome, generally with a lower efficiency. This transformation represents the first example of 5-endo-dig cyclization of 2-alkynylanilines bearing an acyl group linked to the triple bond. By contrast with the previously reported gold-catalyzed reaction of β-(2-aminophenyl)-α,β-ynones, which resulted in the formation of dibenzo[1,5]diazocines through a sequential process triggered by an intermolecular hydroamination, a selective intramolecular anti-Michael hydroamination was observed in the present study by silver/copper catalysis. Density functional theory calculations on the Ag-catalyzed reaction revealed that the catalyst induces an electrostatic arrangement in the TS coherent with the experimentally observed cyclization.

Reaction of 3-(2-nitrophenyl)-1-arylprop-2-en-1-ones with triethylphosphite in microwave revisited: One-pot synthesis of 2-aroylindoles and 2-arylquinolines

One-pot synthesis of 2-aroylindoles and 2-arylquinolines has been achieved by the reductive cyclization of 3-(2-nitrophenyl)-1-arylprop-2-en-1-ones with triethylphosphite [P(OEt)3] under microwave irradiation. The formation of 2-arylquinolines by this method is unprecedented.

N-(2-Aminobenzylidene)-4-methylanilines - stable and cheap alternate for 2-aminobenzaldehydes: concise synthesis of 3-unsubstituted-2-aroylindoles

Abstract Synthesis of 3-unsubstituted-2-aroylindoles starting from readily available N-(2-aminobenzylidene)-4-methylanilines, cheap and stable alternative to 2-aminobenzaldehydes, and α-bromoketones was achieved in moderate to good yields under basic cond

Selective synthesis of quinolines and indoles: Sulfur-assisted or selenium-catalyzed reaction of β-(2-nitrophenyl)-α, β-unsaturated ketones with carbon monoxide

A simple and selective synthetic method of quinolines and indoles by the reaction of β- (2-nitrophenyl)-α,β-unsaturated ketones with carbon monoxide was developed. When β-(2-nitrophenyl)- α,β-unsaturated ketones were allowed to react with carbon monoxide and water in the presence of a stoichiometric amount of sulfur or a catalytic amount of selenium, the corresponding quinolines were produced in moderate-to-good yields. On the other hand, in the absence of water, the indoles were produced by the selenium-catalyzed reaction of the β-(2-nitrophenyl)- α,β-unsaturated ketones with carbon monoxide.

Palladium-catalyzed decarboxylative C2-acylation of indoles with α-oxocarboxylic acids

A palladium-catalyzed decarboxylative C2-acylation of indoles with α-oxocarboxylic acids was achieved. This protocol represents a novel and complementary approach to 2-aroylindoles. The Royal Society of Chemistry 2013.

Synthesis of indoles through highly efficient cascade reactions of sulfur ylides and N-(ortho-chloromethyl)aryl amides

Batting the ylides: A simple procedure carried out under mild conditions allows the direct and efficient synthesis of structurally diverse indoles. This approach involves a cascade reaction of sulfur ylides and N-(ortho-chloromethyl) aryl amides (see scheme). Copyright

A practical synthesis of 2-aroylindoles from N-(2-formylphenyl)trifluoro- acetamides in PEG-400

A one-pot and environmentally benign approach to the synthesis of highly functionalized 3-unsubstituted 2-aroylindoles is described. Moderate to good yields were obtained through the reaction of easily accessible N-(2-formylphenyl)trifluoroacetamides and

Palladium-catalyzed domino C,N-coupling/carbonylation/suzuki coupling reaction: An efficient synthesis of 2-aroyl-/heteroaroylindoles

A convenient one-pot synthesis of 2-aroylindoles using a domino palladium-catalyzed C,N-coupllng/carbonylatlon/C,C-coupling sequence Is described. The reaction Involved easily prepared 2-gem-dibromovinylanilines and boronic acids under carbon monoxide. Op

2,3-substituted indole compounds as anti-inflammatory and analgesic agents

This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alkyl)amino and CN; and n is 0, 1, 2, 3 and 4.This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

AN EFFICIENT SYNTHESIS OF 2-AROYL-1H-INDOLES

2-Aroyl-1H-indoles were directly obtained by the reaction of 1-(N-aroylcarbamoyl)indoles, prepared from 1-(2-oxazolinyl)indole and aroyl chlorides, with LDA.