56436-24-9

Upstream product

• 88-73-3 2-Chloronitrobenzene 
• 109-85-3 2-methoxyethylamine 
• 1493-27-2 ortho-nitrofluorobenzene 
• 7487-88-9 magnesium sulfate 

Downstream Products

• 1338345-12-2 2-[2-(4-chlorophenyl)-1H-imidazol-4-yl]-1-[2-(methyloxy)ethyl]-1H-benzimidazole 
• 405211-51-0 1-(2-Methoxy-ethyl)-1H-benzoimidazol-2-ol 
• 56436-25-0 N¹-(2-methoxyethyl)benzene-1,2-diamine 

Relevant academic research and scientific papers

Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c-MYC Protein Levels in Cells

Elevated expression of the c-MYC oncogene is one of the most common abnormalities in human cancers. Unfortunately, efforts to identify pharmacological inhibitors that directly target MYC have not yet yielded a drug-like molecule due to the lack of any known small molecule binding pocket in the protein, which could be exploited to disrupt MYC function. We have recently described a strategy to target MYC indirectly, where a screening effort designed to identify compounds that can rapidly decrease endogenous c-MYC protein levels in a MYC-amplified cell line led to the discovery of a compound series that phenocopies c-MYC knockdown by siRNA. Herein, we describe our medicinal chemistry program that led to the discovery of potent, orally bioavailable c-MYC-reducing compounds. The development of a minimum pharmacophore model based on empirical structure activity relationship as well as the property-based approach used to modulate pharmacokinetics properties will be highlighted.

Diversity-Oriented Synthesis of Coumarin-Linked Benzimidazoles via a One-Pot, Three-Step, Intramolecular Knoevenagel Cyclization

Diversity-oriented synthesis of coumarin-linked benzimidazoles from N-(2-aminophenyl)-2-cyanoacetamide was achieved via a one-pot, three-step sequential reaction in excellent yields. In situ intramolecular cyclization of the cyanoacetamide afforded benzimidazoles which subsequently underwent a Knoevenagel condensation of the 2-cyanomethylbenzimidazoles with salicylaldehydes promoted by triethylamine to reach the target compounds. An important intermediate, 2-(2-imino-2H-chromen-3-yl)-1H-benzimidazole was characterized by X-ray analysis and further hydrolyzed to 2-(coumarin-3-yl)benzimidazole in acidic condition. Among the synthesized compounds, some were found to be promising inhibitors of porcine kidney d-amino acid oxidase (pkDAO).

Copper catalyzed aerobic oxidative cyclization and ketonization: One pot synthesis of benzoimidazo[1,2-: A] imidazolones

A highly efficient synthesis of benzoimidazo[1,2-a]imidazolone through a novel oxidative 5-exo-dig cyclization-ketonization cascade of 2-aminobenzimidazole, aldehyde and terminal alkyne has been explored under aerobic conditions. The reaction proceeds thr

Renin inhibitors

The invention relates to compounds having the formulae: wherein the variables are as defined herein. The invention further relates to methods of making and using these compounds, and pharmaceutical compositions, kits and articles of manufacture comprise the compounds.

IMIDAZOLYL-IMIDAZOLES AS KINASE INHIBITORS

Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are as defined herein, and methods of making and using the same.

BENZAMIDE DERIVATIVES

Disclosed are benzamide derivatives useful in slowing the expansion of cancer cells.

Synthesis and structure-activity relationship of new piperidinyl and piperazinyl derivatives as antiallergics

A series of piperazinebenzothiazoles 3-5, piperazinebenzimidazoles 6-12, piperidinobenzothiazoles 14-45, piperidinobenzoxazoles 46-52 and piperidinobenzimidazoles 53-129 has been synthesized and their antiallergic activity evaluated by means of the passive cutaneous anaphylaxis (PCA) assay. Structure-activity relationships are discussed and related to classical antihistaminics. Piperidino derivatives with an aryl group linked to the nitrogen atom by an ethyl chain are the most active compounds, with ID50 1 mg/kg po. Some of these compounds are more potent antiallergics than astemizole and terfenadine.

Triazolopyrimidine herbicides

Compounds of the formula: STR1 wherein X, Y and Z are hydrogen, halogen, alkyl, haloalkyl, hydroxy, alkoxyalkyl, alkoxy, haloalkoxy, cycloalkyl, substituted aryl, alkylthio, arylthio, substituted amino or --CO2 R7, wherein R7/s

Oxidative hair dye compositions containing N-substituted o-phenylenediamines and method for their use

Hair dyeing compositions are disclosed which contain an N-substituted o-phenylenediamine, the N-substituent being an alkyl, alkoxyalkyl, hydroxyalkyl, alkylaminoalkyl, dialkylaminoalkyl, phenyl or substituted phenyl. These give reddish shades by purely ox