93-84-5

Usage

Uses

5-Nitro-2-benzimidazolinone is used as intermediates.

InChI:InChI=1/C7H3N3O3/c11-7-8-5-2-1-4(10(12)13)3-6(5)9-7/h1-3H

Upstream product

• 615-16-7 1,3-dihydro-2H-benzimidazol-2-one 
• 5466-84-2 4-nitrophthalic anhydride 
• 99-56-9 4-Nitrophenylene-1,2-diamine 
• 57-13-6 urea 
• 5310-51-0 methyl 2-((2,4-dinitrophenyl)amino)acetate 
• 94-52-0 5-nitrobenzimidazole 
• 616-79-5 2-amino-5-nitro-benzoic acid 
• 97-00-7 1-chloro-2,4-dinitro-benzene 
• 35411-68-8 ethyl N-(2,4-dinitrophenylcarbamate) 
• 1202680-24-7 phenyl 4,5-dichloro-6-oxopyridazine-1(6H)-carboxylate 
• 70297-88-0 2,4-Dinitrophenylharnstoff 
• 530-62-1 1,1'-carbonyldiimidazole 
• 1192307-15-5 methyl 2-iodo-4-nitrophenylcarbamate 
• 70254-61-4 4-hydroxy-6-methyl-2H-pyran-2-one 

Downstream Products

• 5955-72-6 2-chloro-5-nitro-1H-benzo[d]imidazole 
• 95-23-8 5-amino-1,3-dihydro-benzoimidazol-2-one 
• 3705-86-0 5,6-dinitro-2,3-dihydro-1H-benzimidazol-2-one 
• 925220-86-6 1,3-diisopropyl-5-nitro-1H-benzo[d]imidazole-2(3H)-one 
• 50796-10-6 4,5,6-trinitro-2,3-dihydro-1H-benzimidazol-2-one 
• 1334919-26-4 1-(1,3-dibenzyl-2-oxo-1,3-dihydrobenzimidazol-5-yl)-2,6-dimethylpyridin-4-one 
• 928711-32-4 5-amino-1,3-dibenzyl-1,3-dihydrobenzimidazol-2-one 
• 1334919-19-5 1,3-dibenzyl-1,3-dihydro-5-(pyrrol-1-yl)-benzimidazol-2-one 
• 53439-88-6 5-amino-1,3-dimethyl-1,3-dihydro-2H-benzo[d]imidazol-2-one 
• 55327-66-7 1,3-dibenzyl-5-nitro-1,3-dihydrobenzimidazol-2-one 

Relevant academic research and scientific papers

Oxidative Cyclization-Induced Activation of a Phosphoinositide 3-Kinase Inhibitor for Enhanced Selectivity of Cancer Chemotherapeutics

In this work, we designed a prodrug that reacts with cellular oxidative equivalents leading to ether cleavage and cyclization to release an active phosphatidylinositol 3-kinase (PI3K) inhibitor. We show that the compound reduces affinity for PI3KA relative to the PI3K inhibitor, is slow to intercellularly oxidize, and is resistant to liver microsomes. We observed modest activity in untreated acute myeloid leukemia cells and 14-fold selectivity relative to non-cancerous cells. The cellular activity of the compound can be modulated by the addition of antioxidants or oxidants, indicating the compound activity is sensitive to cellular reactive oxygen species (ROS) state. Co-treatment with cytosine arabinoside or doxorubicin was used to activate the compound inside cells. We observed strong synergistic activity specifically in acute myeloid leukemia (AML) cancer cells with an increase in selective anticancer activity of up to 90-fold. Thus, these new self-cyclizing compounds can be used to increase the selectivity of anticancer agents.

Method for synthesizing benzothiazolone-based and 1,3-disubstituted urea-based derivatives through activation of CO2

The present invention relates to a method for synthesizing benzothiazolone-based and 1,3-disubstituted urea-based derivatives through activation of CO2. According to the present invention, an inexpensive and easily-available sulfur-containing metal salt compound is first used as an activation catalyst for CO2, and a reaction raw material and CO2 are converted into a corresponding target compound at a low reaction temperature under a low CO2 pressure; and the method has high atomic economy, can reduce the generation of by-products, meets the standards of environmental friendliness and environmentally friendly chemistry, and is the effective way capable of completely utilizing CO2 as the renewable resource, developing new energy and achieving the beneficial cycle of carbon in nature.

Sulfated polyborate-catalyzed efficient and expeditious synthesis of (un)symmetrical ureas and benzimidazolones

The excellent catalytic potential of sulfated polyborate is utilized in the synthesis of (un)symmetrical ureas and benzimidazolones by heating amines or substituted OPDA and urea or N-phenylureas under a solvent-free condition at 120 °C is described. The key advantages of the present protocol are phosgene-free, and other hazardous reagents or organic solvent free, high reaction rates and yields, simple workup procedure, and recyclability of the catalyst.

BROMODOMAIN INHIBITORS FOR TREATING DISEASE

Disclosed herein are compounds and compositions useful in the treatment of bromodomain-containing protein-mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibiting activity of a bromodomain-containing protein in a human or animal subject are also provided.

Facile Synthesis of Benzo[ d ]azol-2(3 H)-ones Using 2-Phenoxycarbonyl-4,5-dichloropyridazin-3(2 H)-one as Green CO Source

Developing eco-friendly, stable, and easy-to-handle acyl sources is of great importance in synthetic and green chemistry. This study describes the synthesis of benzo[d]azol-2(3H)-ones such as benzo[d]thiazol-2(3H)-ones, benzo[d]oxazol-2(3H)-ones, and benzo[d]imidazol-2(3H)-ones using 2-phenoxycarbonyl-4,5-dichloropyridazin-3(2H)-one in one pot. The reaction reported is carried out under neutral or acidic conditions in the presence of zinc or sodium bicarbonate to give the corresponding heterocycles in good to excellent yields. The reaction uses a solid stable carbonyl source that is a recyclable functional-group carrier, pyridazin-3(2H)-one.

COMPOUNDS USEFUL AS ANTIBIOTIC TOLERANCE INHIBITORS

The disclosure provides compounds and pharmaceutical compositions of the compounds useful for treating chronic and acute bacterial infections. Certain of the compounds are compounds and salts of general Formula VIII Certain compounds of this disclosure are MvfR inhibitors. MvfR inhibitors reduce the formation of antibiotic tolerant bacterial strains and are useful for treating Gram-negative bacterial infections and reducing the virulence of Pseudomonas aeruginosa. Methods of treating bacterial infections in a patient, including Pseudomonas aeruginosa infections, are also provided by the disclosure.

Preparation of 2(3H)-benzimidazolone and its derivative under aqueous condition as a potential agent for antidiabetic compounds

A focused library of 2(3H)-benzimidazolone and its derivatives has been synthesized in an attempt to identify their antidiabetic potential. All the products have been synthesized under aqueous conditions in lesser time with better yield and purity. A new effective and convenient method for in situ synthesis of five member heterocyclic ring by reaction of phenylene diamine with urea in solvent phase. All the synthesized compounds were characterized by modern spectroscopic techniques.

DBU-based ionic-liquid-catalyzed carbonylation of o-phenylenediamines with CO2 to 2-benzimidazolones under solvent-free conditions

Herein, a new route was presented to synthesize 2-benzimidazolones via the carbonylation of o-phenylenediamines with CO2 catalyzed by 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU)-based ionic liquids under solvent-free conditions. DBU acetate ([DBUH][OAc]) displayed high efficiency for catalyzing the reactions of CO2 with o-phenylenediamines, and a series of benzimidazolones were obtained in high yields. It was demonstrated that [DBUH][OAc] could serve as a bifunctional catalyst for these reactions with the cation activating CO2 and the anion activating o-phenylenediamines. This protocol provides an effective and environmentally friendly alternative route for production of benzimidazolones, and extends the chemical utilization of CO2 in organic synthesis as well.

A bifunctional tungstate catalyst for chemical fixation of CO2 at atmospheric pressure

No pressure: A simple monomeric tungstate, [WO4]2-, serves as a highly efficient homogeneous catalyst for various transformations of CO2 at atmospheric pressure. The tungsten-oxo moiety activates CO2 and the substrate simultaneously. The catalyst system is high yielding and applicable to a wide range of substrates such as amines (see scheme), 2-aminobenzonitriles, and propargylic alcohols. Copyright

2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.