5228-61-5

Usage

Uses

Used in Pharmaceutical Synthesis:
5-bromo-2-nitrobenzenamine is utilized as an intermediate in the production of pharmaceuticals, playing a crucial role in the synthesis of various medicinal compounds due to its unique chemical structure and reactivity.
Used in Agrochemical Production:
In the agrochemical industry, 5-bromo-2-nitrobenzenamine serves as an intermediate, contributing to the development of products designed to enhance crop protection and management.
Used in Dye Manufacturing:
5-bromo-2-nitrobenzenamine is also employed in the manufacturing of dyes, where its chemical properties allow for the creation of a range of colorants used in different industries.
Used in Organic Chemical Reactions:
5-bromo-2-nitrobenzenamine has been studied for its potential use in organic chemical reactions, where it may act as a reagent to facilitate specific transformations or syntheses.
Used as a Reagent in Organic Synthesis:
As a reagent, 5-bromo-2-nitrobenzenamine is valuable in organic synthesis for its ability to participate in a variety of chemical processes, aiding in the construction of complex organic molecules.

Upstream product

• 51686-78-3 2,4-dibromonitrobenzene 
• 586-78-7 para-nitrophenyl bromide 
• 7664-93-9 sulfuric acid 
• 591-19-5 m-Bromoaniline 
• 621-38-5 3-bromoacetanilide 
• 64-19-7 acetic acid 
• 343864-78-8 4-bromo-2-iodo-1-nitrobenzene 
• 7664-41-7 ammonia 
• 367-24-8 4-bromo-2-fluoroaniline 
• 106-37-6 1.4-dibromobenzene 
• 321-23-3 4-bromo-2-fluoronitrobenzene 
• 593-56-6 N-methoxylamine hydrochloride 
• 108-36-1 1,3-dibromobenzene 
• 873983-28-9 (3-amino-4-nitro-phenyl)-arsonic acid 

Downstream Products

• 20691-71-8 5-(dimethylamino)-2-nitroaniline 
• 89465-97-4 4-bromo-2-chloro-1-nitrobenzene 
• 105971-15-1 5-bromo-2-nitro-biphenyl 
• 75293-97-9 2-nitro-4,5-dibromoaniline 
• 343864-78-8 4-bromo-2-iodo-1-nitrobenzene 
• 586-78-7 para-nitrophenyl bromide 
• 1575-37-7 4-Bromo-benzene-1,2-diamine 
• 1552-17-6 2-nitro-5-phenoxyaniline 
• 849235-53-6 2-nitro-5-thiophen-2-yl-phenylamine 
• 76129-28-7 4-nitrobiphenyl-3-ylamine 
• 63019-99-8 4-dimethylamino-2-(phenylamino)nitrobenzene 
• 129195-09-1 5-(N,N-dimethylamino)-2-nitroacetamide 
• 63019-87-4 acetic acid-(2-anilino-4-dimethylamino-anilide) 
• 626-39-1 1,3,5-trisbromobenzene 

Relevant academic research and scientific papers

Sulfide Analogues of Flupirtine and Retigabine with Nanomolar KV7.2/KV7.3 Channel Opening Activity

The potassium channel openers flupirtine and retigabine have proven to be valuable analgesics or antiepileptics. Their recent withdrawal due to occasional hepatotoxicity and tissue discoloration, respectively, leaves a therapeutic niche unfilled. Metabolic oxidation of both drugs gives rise to the formation of electrophilic quinones. These elusive, highly reactive metabolites may induce liver injury in the case of flupirtine and blue tissue discoloration after prolonged intake of retigabine. We examined which structural features can be altered to avoid the detrimental oxidation of the aromatic ring and shift oxidation toward the formation of more benign metabolites. Structure–activity relationship studies were performed to evaluate the KV7.2/3 channel opening activity of 45 derivatives. Sulfide analogues were identified that are devoid of the risk of quinone formation, but possess potent KV7.2/3 opening activity. For example, flupirtine analogue 3-(3,5-difluorophenyl)-N-(6-(isobutylthio)-2-(pyrrolidin-1-yl)pyridin-3-yl)propanamide (48) has 100-fold enhanced activity (EC50=1.4 nm), a vastly improved toxicity/activity ratio, and the same efficacy as retigabine in vitro.

A preparation method of a dog or CAT

The invention discloses a dog or CAT a kind of preparation method. Characterized in that (1) in order to inter-bromobenzene as the starting material, nitric acid/sulfuric acid system through the nitration reaction, process for preparing the intermediate 1 (2, 4 - dibromo nitrobenzene); (2) using the intermediate 1 as raw materials, through the ammonia in methanol solution of ammoniation reaction, to prepare the intermediate 2 (5 - bromo - 2 - nitroaniline); (3) using the intermediate 2 and thiophenol sodium solution as raw materials, through the condensation reaction, process for preparing the intermediate 3 (4 - phenylthio - 2 - nitroaniline); (4) intermediate 3 through the palladium catalytic hydrogenation reduction, to produce intermediate 4 (4 - phenylthio - 1, 2 - phenylenediamine); (5) intermediate 4 and melamine-based methyl formate solution, through the cyclization reaction, the profuse benzene reaches zuo generating products. The method clean environment, the production cost is low, with a purity of 99.5% or more, the yield is not lower than 84.0%.

Importance of 5/6-aryl substitution on the pharmacological profile of 4?-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1?-biphenyl]-2-carboxylic acid derived PPARγ agonists

In this structure-activity relationship study, the influence of aryl substituents at position 5 or 6 on the pharmacological profile of the partial PPARγ agonist 4‘-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1‘-biphenyl]-2-carboxylic acid was investigated. This lead was previously identified as the essential part of telmisartan to induce PPARγ activation. Para-OCH3-phenyl substitution strongly increased potency and efficacy independent of the position. Both compounds represent full agonists because of strong hydrophobic contacts with the amino acid Phe363 in the ligand binding domain. Partial agonists with higher potency than telmisartan or the lead were obtained with OH or Cl substituents at the phenyl ring. Molecular modeling suggested additional hydrogen or halogen bonds with Phe360 located at helix 7. It is assumed that these interactions fix helix 7, thereby promoting a partial agonist conformation of the receptor. The theoretical considerations correlate very well with the results from the luciferase transactivation assay using hPPARγ-LBD as well as those from a time-resolved fluorescent resonance energy transfer (TR-FRET) assay in which the coactivator (TRAP220, PGC-1α) recruitment and corepressor (NCoR1) release pattern was investigated.

NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), (II-ii), (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

TNF -Alpha Modulating Benzimidazoles

A series of benzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

BENZOTRIAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY

A series of substituted benzotriazole derivatives, being potent modulators of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

The development of benzimidazoles as selective rho kinase inhibitors

Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC50 10 nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).

Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties

Herein we report investigations into the p38α MAP kinase activity of trisubstituted imidazoles that led to the identification of compounds possessing highly potent in vivo activity. The SAR of a novel series of imidazopyridines is demonstrated as well, resulting in compounds possessing cellular potency and enhanced in vivo activity in the rat collagen-induced arthritis model of chronic inflammation.