4487-57-4

Basic information

• Product Name: 2,4-DIBROMO-5-NITROPYRIDINE
• Synonyms: 2,4-DIBROMO-5-NITROPYRIDINE;2,4-DibroMo-5-nitropyridine DISCONTINUED;Pyridine,2,4-dibromo-5-nitro-
• CAS NO: 4487-57-4
• Molecular Formula: C₅H₂Br₂N₂O₂
• Molecular Weight: 281.89
• EINECS: 213-580-7
• Product Categories: Pyridine series;Aromatics;Heterocycles;Intermediates;Heterocycle-Pyridine series
• Mol File: 4487-57-4.mol
• Article Data: 10

Chemical Properties

• Melting Point: 99 °C
• Boiling Point: 292 °C at 760 mmHg
• Flash Point: 130.4 °C
• Appearance: /
• Density: 2.221 g/cm³
• Vapor Pressure: 0.0033mmHg at 25°C
• Refractive Index: 1.649
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• PKA: -2.18±0.10(Predicted)
• CAS DataBase Reference: 2,4-DIBROMO-5-NITROPYRIDINE(CAS DataBase Reference)
• NIST Chemistry Reference: 2,4-DIBROMO-5-NITROPYRIDINE(4487-57-4)
• EPA Substance Registry System: 2,4-DIBROMO-5-NITROPYRIDINE(4487-57-4)

Safety Data

• Hazardous Substances Data: 4487-57-4(Hazardous Substances Data)

Usage

Uses

2,4-Dibromo-5-nitropyridine is a tri-substituted pyridine derivative used in the preparation of AKT kinase inhibitors and antihypertensive agents.

InChI:InChI=1/C5H2Br2N2O2/c6-3-1-5(7)8-2-4(3)9(10)11/h1-2H

Upstream product

• 13091-23-1 4-chloro-3-nitropyridine 
• 850663-54-6 4-chloro-2-hydroxy-5-nitropyridine 
• 31872-62-5 4-methoxy-3-nitro-pyridine 
• 607373-82-0 2-hydroxy-4-methoxy-5-nitro pyridine 

Downstream Products

• 1449669-27-5 2-bromo-5-nitro-4-vinylpyridine 
• 1449669-28-6 2-(1-methyl-1H-pyrazol-4-yl)-5-nitro-4-vinylpyridine 
• 1449669-29-7 4-ethyl-6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-ylamine 
• 1449669-30-0 N-(4-ethyl-6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)-1-methyl-1H-imidazo[4,5-c]pyridin-6-amine 
• 1449665-20-6 N-(4-ethyl-6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)-N,1-dimethyl-1H-imidazo[4,5-c]pyridin-6-amine 
• 1612171-82-0 (2-bromo-5-nitropyridin-4-yl)isopropylamine 
• 1612172-37-8 4-[4-(1-isopropyl-1H-imidazo[4,5-c]pyridin-6-ylamino)pyrimidin-2-yl]piperidine-1-carboxylic acid tert-butyl ester 
• 1612172-38-9 4-[4-(1-isopropyl-1H-imidazo[4,5-c]pyridin-6-ylamino)pyrimidin-2-yl]-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester 
• 1612172-39-0 4-[4-(1-isopropyl-1H-imidazo[4,5-c]pyridin-6-ylamino)pyrimidin-2-yl]-1,2,3,6-tetrahydropyridinium chloride 
• 1612164-36-9 (1-isopropyl-1H-imidazo[4,5-c]pyridin-6-yl)-[2-(1-methanesulfonyl-1,2,3,6-tetrahydropyridin-4-yl)pyrimidin-4-yl]amine 
• 1612164-37-0 (1-isopropyl-1H-imidazo[4,5-c]pyridin-6-yl)-(2-morpholin-4-ylpyrimidin-4-yl)amine 
• 1612164-51-8 N⁴-(1-isopropyl-1H-imidazo[4.5-c]pyridin-6-yl)-N²-(1H-pyrazol-4-yl)pyrimidine-2,4-diamine 
• 1612164-52-9 1-isopropyl-N-(2-(4-(trifluoromethoxy)piperidin-1-yl)pyrimidin-4-yl)-1H-imidazo[4,5-c]pyridin-6-amine 
• 1612172-56-1 benzyl N-((1R,5S,6s)-3-(4-((1-isopropyl-1H-imidazo[4,5-c]pyridin-6-yl)amino)pyrimidin-2-yl)-3-azabicyclo[3.1.0]hexan-6-yl)carbamate 

Relevant articles and documents

EGFR PROTEOLYSIS TARGETING CHIMERIC MOLECULES AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Because of their increased activity against activating mutants, first-generation epidermal growth factor receptor (EGFR) kinase inhibitors have had remarkable success in treating non-small-cell lung cancer (NSCLC) patients, but acquired resistance, through a secondary mutation of the gatekeeper residue, means that clinical responses only last for 8-14 months. Addressing this unmet medical need requires agents that can target both of the most common double mutants: T790M/L858R (TMLR) and T790M/del(746-750) (TMdel). Herein we describe how a noncovalent double mutant selective lead compound was optimized using a strategy focused on the structure-guided increase in potency without added lipophilicity or reduction of three-dimensional character. Following successive rounds of design and synthesis it was discovered that cis-fluoro substitution on 4-hydroxy- and 4-methoxypiperidinyl groups provided synergistic, substantial, and specific potency gain through direct interaction with the enzyme and/or effects on the proximal ligand oxygen atom. Further development of the fluorohydroxypiperidine series resulted in the identification of a pair of diastereomers that showed 50-fold enzyme and cell based selectivity for T790M mutants over wild-type EGFR (wtEGFR) in vitro and pathway knock-down in an in vivo xenograft model.

IMIDAZO [4, 5 -C] PYRIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein. Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.