36798-24-0

Usage

Derivative of indole

A heterocyclic organic compound commonly found in natural products

Carbonitrile group

Located at the 5-position of the indole ring, gives unique chemical properties and reactivity

Building block

Widely used in the synthesis of pharmaceuticals, agrochemicals, and other fine chemicals

Versatile nature

Ability to undergo various chemical transformations to yield complex and diverse molecular structures

Potential biological activity

Being studied for its potential therapeutic applications

Upstream product

• 1075-35-0 5-chloro-2-methylindole 
• 57-13-6 urea 
• 1075-34-9 5-bromo-2-methyl-1H-indole 
• 124-38-9 carbon dioxide 
• 67-64-1 acetone 
• 873-74-5 4-Aminobenzonitrile 
• 15861-24-2 1H-indole-5-carbonitrile 
• 144340-21-6 1-benzenesulfonyl-1H-indole-5-carbonitrile 
• 1240112-40-6 1-benzenesulfonyl-2-methyl-1H-indole-5-carbonitrile 

Downstream Products

• 1383843-46-6 methyl 1-(4-chlorobenzyl)-2-methyl-1H-indole-5-carboxylate 
• 1383924-68-2 (1-(4-chlorobenzyl)-2-methyl-1H-indol-5-yl)methanol 
• 1383924-69-3 (1-(4-chlorobenzyl)-2-methyl-1H-indol-5-yl)methyl acetate 
• 1383924-71-7 1-(4-chlorobenzyl)-5-(methoxymethyl)-2-methyl-1H-indole 
• 1383924-79-5 1-(4-chlorobenzyl)-2-methyl-1H-indole-5-carboxamide 
• 1383923-08-7 2-(1-(4-chlorobenzyl)-5-cyano-2-methyl-1H-indol-3-yl)-N-(2-methoxypyridin-4-yl)-2-oxoacetamide 
• 1383924-87-5 tert-butyl 1-(4-chlorobenzyl)-2-methyl-1H-indol-5-ylcarbamate 
• 1383924-88-6 tert-butyl 1-(4-chlorobenzyl)-2-methyl-1H-indol-5-yl(methyl)carbamate 
• 1383924-44-4 1-(4-chlorobenzyl)-2-methyl-1H-indole-5-carbonitrile 
• 36798-25-1 5-Aminomethyl-2-methylindol 
• 671215-52-4 2-Methyl-1H-indole-5-carbaldehyde 

Relevant academic research and scientific papers

Reductive cyanation of organic chlorides using CO2 and NH3 via Triphos–Ni(I) species

Cyano-containing compounds constitute important pharmaceuticals, agrochemicals and organic materials. Traditional cyanation methods often rely on the use of toxic metal cyanides which have serious disposal, storage and transportation issues. Therefore, there is an increasing need to develop general and efficient catalytic methods for cyanide-free production of nitriles. Here we report the reductive cyanation of organic chlorides using CO2/NH3 as the electrophilic CN source. The use of tridentate phosphine ligand Triphos allows for the nickel-catalyzed cyanation of a broad array of aryl and aliphatic chlorides to produce the desired nitrile products in good yields, and with excellent functional group tolerance. Cheap and bench-stable urea was also shown as suitable CN source, suggesting promising application potential. Mechanistic studies imply that Triphos-Ni(I) species are responsible for the reductive C-C coupling approach involving isocyanate intermediates. This method expands the application potential of reductive cyanation in the synthesis of functionalized nitrile compounds under cyanide-free conditions, which is valuable for safe synthesis of (isotope-labeled) drugs.

Cyaniding method for preparing nitrile compound

The invention provides a cyaniding method for preparing a nitrile compound. Organic halide or pseudohalide, CO2 and NH3 which are low in price and are easily obtained and a reducing agent react, a selective cyaniding reaction is conducted in the presence of a transition metal catalyst, and the target product namely organic the nitrile compound is obtained. According to the cyaniding method for preparing the nitrile compound, a new reaction route is used, through a CO2 and NH3 reaction of metal catalysis, dehalogenation cyaniding or quasi halide cyaniding of halide or pseudohalide is directly achieved through a one-pot method, the problem is solved that a traditional cyanation reaction needs equivalent toxic cyanide, a new direct and convenient method for preparing isotope-labeled nitrile compounds is provided at the same time, and the method can be applied to medicine, tracing, biology and medicine research and development.

PROTEASOME ACTIVITY ENHANCING COMPOUNDS

The present invention is directed to compounds having the Formula (I), (II), (III), (IV), and (V), compositions thereof, the methods of synthesis of the compouds of interest, and to methods for the treatment of a condition associated with a dysfunction in proteostasis, such as cancer, inflammatory conditions, neurodegeneration, metabolic conditions, comprising administering an effective amount of a compound of the invention.

Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

The AAA-ATPase p97 plays vital roles in mechanisms of protein homeostasis, including ubiquitin-proteasome system (UPS) mediated protein degradation, endoplasmic reticulum-associated degradation (ERAD), and autophagy. Herein we describe our lead optimization efforts focused on in vitro potency, ADME, and pharmaceutical properties that led to the discovery of a potent, ATP-competitive, D2-selective, and orally bioavailable p97 inhibitor 71, CB-5083. Treatment of tumor cells with 71 leads to significant accumulation of markers associated with inhibition of UPS and ERAD functions, which induces irresolvable proteotoxic stress and cell death. In tumor bearing mice, oral administration of 71 causes rapid accumulation of markers of the unfolded protein response (UPR) and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. 71 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors.

NEW POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTOR

The present invention relates to indole derivatives useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said com- pounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.

Positive allosteric modulators of nicotinic acetylcholine receptor

The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.

FAAH INHIBITORS

The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the com

NOVEL COMPOUNDS EFFECTIVE AS XANTHINE OXIDASE INHIBITORS, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same.

AMIDE DERIVATIVE OR SALT THEREOF

[Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for

DPP IV inhibitors

The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.