851514-65-3

Upstream product

• 603-76-9 1-methylindole 
• 614-16-4 Benzoylacetonitrile 
• 582-24-1 1-phenyl-2-hydroxyethanone 
• 61040-96-8 β-hydroperoxybenzeneethanol 
• 100-42-5 styrene 
• 122-78-1 phenylacetaldehyde 
• 25726-04-9 phenylglyoxylyl chloride 
• 611-73-4 Benzoylformic acid 
• 33288-26-5 1-(1H-indol-3-yl)-2-phenylethane-1,2-dione 
• 74-88-4 methyl iodide 
• 1075-06-5 2,2-dihydroxy-1-phenyl-ethanone 
• 98-86-2 acetophenone 
• 1074-12-0 phenylglyoxal hydrate 
• 32119-53-2 N-methyl-N-phenacylaniline 

Downstream Products

• 1364917-78-1 2-(1-methyl-1H-indol-3-yl)-3-phenylquinoxaline 

Relevant academic research and scientific papers

Novel positive allosteric modulators of A2B adenosine receptor acting as bone mineralisation promoters

Small-molecules acting as positive allosteric modulators (PAMs) of the A2B adenosine receptor (A2B AR) could potentially represent a novel therapeutic strategy for pathological conditions characterised by altered bone homeostasis, including osteoporosis. We investigated a library of compounds (4-13) exhibiting different degrees of chemical similarity with three indole derivatives (1-3), which have been recently identified by us as PAMs of the A2B AR able to promote mesenchymal stem cell differentiation and bone formation. Evaluation of mineralisation activity of 4-13 in the presence and in the absence of the agonist BAY60-6583 allowed the identification of lead compounds with therapeutic potential as anti-osteoporosis agents. Further biological characterisation of one of the most performing compounds, the benzofurane derivative 9, confirmed that such a molecule behaves as PAM of the A2B AR.

KI-Promoted Oxidative Coupling of Styrenes with Indoles under Metal-Free Conditions: Facile Access to C-3 Dicarbonyl Indoles

A new and efficient method for the synthesis of C-3 dicarbonyl indoles via oxidative cross-coupling of styrenes with indoles under metal-free conditions has been developed. Moreover, a broad scope of C-3 dicarbonyl indoles in moderate to good yields were obtained, and a plausible mechanism is proposed based on control and isotope-labeling experiments.

Synthesis method of double-carbonyl indole compounds

The invention discloses a synthesis method of double-carbonyl indole compounds. The synthesis method comprises the following steps of performing oxidization coupling reaction on acetaldehyde derivatives I and indole derivatives II to obtain the double-car

Dual Role of H2O2 in Palladium-Catalyzed Dioxygenation of Terminal Alkenes

A palladium-catalyzed, environmentally friendly dioxygenation reaction of simple alkenes has been developed that enabled rapid assembly of valuable α-hydroxy ketones with high atom economy. Notably, control experiments and 18O isotope-labeling experiments established that H2O2 played a dominant dual role in this transformation.

A double-carbonyl indole compounds and its synthetic method

The present invention discloses a method for double carbonylation of indole, wherein alpha-hydroxyketone and indole are adopted as reaction raw materials, oxygen is adopted as an oxidizing agent, and a reaction is performed in benzene at a temperature of 80 DEG C under the effect of a copper catalyst to obtain the bis carbonyl indole compound represented by a formula (III). According to the present invention, advantages of high efficiency of the reaction, high yield, application of the oxygen as the oxidizing agent, mild reaction conditions, no requirement of strong acid and strong alkali, catalysis with the cheap metal, easy reaction substrate preparation, and reaction amplification achieving are provided.

Synthesis of 3-acylated indoles through iron-catalyzed oxidative coupling of indoles with α-amino carbonyl compounds

A novel iron-catalyzed oxidative coupling of indoles with α-amino carbonyl compounds has been developed. The transformation provides an attractive approach to the synthesis of 3-acylindoles, with the advantages of easily available starting materials and high functional group tolerance. Furthermore, control experiments imply that a radical process maybe involved in this reaction.

Method for continuously preparing dicarbonyl indole compound by utilizing micro-channel reaction device

The invention relates to a method for continuously preparing a dicarbonyl indole compound by utilizing a micro-channel reaction device. A phenylacetaldehyde compound I and an indole compound II are used as reaction raw materials, and in an iodine/dimethyl sulfoxide oxidation system, a continuous two-step reaction is performed in the micro-channel reaction device to obtain the dicarbonyl indole compound III; the reaction process is as shown in a reaction formula: (with reference to the specification). The method disclosed by the invention is simple, convenient, safe and efficient to operate and mild in reaction condition, has excellent substrate universality and also can be implemented after reaction amplification.

3-dicarbonyl substitution indole compound and preparation method thereof

The invention discloses a 3-dicarbonyl substitution indole compound and a preparation method thereof, and belongs to the technical field of synthesis of indole derivatives. According to the technical scheme, the 3-dicarbonyl substitution indole compound i

The dicarbonylation of indoles: Via Friedel-Crafts reaction with dicarbonyl nitrile generated in situ and retro-cyanohydrination

A novel one-pot tandem reaction of indole and β-carbonyl nitrile to generate dicarbonyl indoles has been developed. This tandem process involves α-oxonation of the β-carbonyl nitrile to afford α,β-dicarbonyl nitrile, Friedel-Crafts reaction with indoles and subsequent retro-cyanohydrination of cyano tertiary alcohol form dicarbonyl indoles.

Direct Regioselective Oxidative Cross-Coupling of Indoles with Methyl Ketones: A Novel Route to C3-Dicarbonylation of Indoles

The first C3-dicarbonylation of indoles was realized through direct oxidative cross-coupling of indoles with methyl ketones in the presence of molecular iodine and pyrrolidine. This reaction constructed a highly efficient indolyl diketones scaffold, which