95306-87-9

Upstream product

• 4264-35-1 2-acetylindole 
• 100-44-7 benzyl chloride 
• 17017-71-9 1-benzyl-1H-indole-2-carboxylic acid 
• 917-54-4 methyllithium 
• 3770-50-1 2-carbethoxyindole 
• 100-39-0 benzyl bromide 
• 17017-66-2 ethyl 1-benzyl-1H-indole-2-carboxylate 
• 75-16-1 methylmagnesium bromide 

Downstream Products

• 175441-65-3 1-{5-Acetyl-4-[2-(1-benzyl-1H-indol-2-yl)-2-oxo-ethyl]-1-methyl-1,4-dihydro-pyridin-3-yl}-2,2,2-trichloro-ethanone 
• 175441-66-4 5-Acetyl-4-[2-(1-benzyl-1H-indol-2-yl)-2-oxo-ethyl]-1-methyl-1,4-dihydro-pyridine-3-carboxylic acid methyl ester 

Relevant academic research and scientific papers

Catalytic Enolate Arylation with 3-Bromoindoles Allows the Formation of β-Carbolines

Synthesis of substituted β-carbolines was accomplished by utilizing the catalytic enolate arylation reaction of ketones in conjunction with several 3-bromoindole derivatives. Quenching of the arylation reaction in situ with an electrophile allowed ready i

4-carbonyl-2-butene acid compound and use thereof

The invention provides a 4-carbonyl-2-butene acid compound with good inhibition activity against PA_N. The compound has a general formula (I), wherein R1 represents C1-C4 alkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; and R2 represents hydroxy or substituted amino. The invention also relates to a medicine composition with the compound as an active component, and an application of the compound and the medicine composition provided by the invention in treating influenza.

Design and synthesis of novel indole β-diketo acid derivatives as HIV-1 integrase inhibitors

Diketo acids such as S-1360 (1A) and L-731,988 (2) are potent and selective inhibitors of HIV-1 integrase (IN). A plethora of diketo acid-containing compounds have been claimed in patent literature without disclosing much biological activities and synthetic details (reviewed in Neamati, N. Exp. Opin. Ther. Pat. 2002, 12, 709-724). To establish a coherent structure - activity relationship among the substituted indole nucleus bearing a β-diketo acid moiety, a series of substituted indole-β-diketo acids (4a-f and 5a-e) were synthesized. All compounds tested showed anti-IN activity at low micromolar concentrations with varied selectivity against the strand transfer process. Three compounds, the indole-3-β-diketo acids 5a and 5c, and the parent ester 9c, have shown an antiviral activity in cell-based assays. We further confirmed a keto-enolic structure in the 2,3-position of the diketo acid moiety of a representative compound (4c) using NMR and X-ray crystallographic analysis. Using this structure as a lead for all of our computational studies, we found that the title compounds extensively interact with the essential amino acids on the active site of IN.

Reaction of indole-2,3-dicarboxylic anhydride with grignard reagents: synthesis of 2-acylindoles

Reaction of indole-2,3-dicarboxylic anhydride with methylmagnesium bromide and phenylmagnesium bromide gave 2-acetyl- and 2-benzoyl-indole-3-carboxylic acids, but with tert-butylmagnesium chloride, 3-pivaloylindole-2-carboxylic acids were obtained as the main products. Treatment of 2-acylindole-3-carboxylic acids with copper chromite in quinoline or potassium hydroxide gave the corresponding 2-acylindoles.