577-72-0

Usage

InChI:InChI=1/C7H8N2O3/c1-12-7-3-2-5(8)4-6(7)9(10)11/h2-4H,8H2,1H3

Upstream product

• 119-27-7 2,4-dinitroanisole 
• 50651-39-3 2-nitro-4-acetylamino-anisole 
• 51-66-1 4-methoxyacetanilide 
• 104-94-9 4-methoxy-aniline 
• 121-44-8 triethylamine 
• 89-41-8 4-methoxy-3-nitrobenzoic acid 
• 7664-93-9 sulfuric acid 
• 67-56-1 methanol 
• 364-76-1 4-Fluoro-3-nitroaniline 
• 124-41-4 sodium methylate 
• 155863-54-0 p-methoxyanilinium nitrate 
• 119-34-6 4-amino-2-nitrophenol 
• 74-88-4 methyl iodide 
• 97-00-7 1-chloro-2,4-dinitro-benzene 

Downstream Products

• 29906-33-0 4-diazo-2-nitrophenol 
• 91-23-6 2-Nitroanisole 
• 52692-09-8 4-iodo-2-nitroanisole 
• 88-75-5 2-hydroxynitrobenzene 
• 228425-51-2 N-(4-methoxy-3-nitro-phenyl)-N'-phenyl-urea 
• 77600-77-2 propionic acid-(4-methoxy-3-nitro-anilide) 
• 6623-91-2 6-methoxy-5-nitroquinoline 
• 855760-37-1 6-methoxy-7-nitro-quinoline 
• 23745-12-2 Cyclopropanecarboxylic acid (4-methoxy-3-nitro-phenyl)-amide 
• 89-21-4 4-chloro-2-nitroanisole 
• 195534-11-3 4-methoxy-3-nitro-1-pentafluorophenylsulfonamidobenzene 
• 33696-00-3 4-bromo-1-methoxy-2-nitrobenzene 
• 308338-38-7 [2-benzyloxy-1-(2-methoxy-5-pentafluorobenzenesulfonylamino-phenylcarbamoyl)-ethyl]-carbamic acid tert-butyl ester 
• 374778-38-8 (1S,2R)-[2-benzyloxy-1-(2-methoxy-5-pentafluorobenzenesulfonylaminophenylcarbamoyl)propyl]carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of quinazoline derivatives as dual HDAC1 and HDAC6 inhibitors for the treatment of cancer

Fifty-eight quinazoline-based compounds were designed and synthesized based on the structural optimizations from the lead compound 23bb in an attempt to search for more potent dual HDAC1 and HDAC6 inhibitors. Among them, 32c (HDAC1, IC50?=?31.1

2 - Amino - 4 - acetamido anisole novel synthesis process (by machine translation)

The present invention provides a novel 2 - amino - 4 - acetamido anisole synthesis process, the usage of palladium bi-metal catalysts and the palladium/carbon catalyst to replace Rany - Ni catalyst, to the anisole on the nitro-selective catalytic hydrogenation, which not only reduces use Rany - Ni catalyst of post-industrial risks, while at the same time, the resulting 2 - amino - 4 - acetyl anisole purity higher, greater yield. (by machine translation)

Preparation method for osimertinib mesylate

The invention discloses a preparation method for osimertinib mesylate. The chemical name of osimertinib mesylate is N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide mesylate (AZD9291), and the chemical formula is C28H33N7O2.CH4O3S. The process of the preparation technique of the preparation method is simple, materials areeasy to obtain, and the preparation method is cost-efficient and environment-friendly, can help realize industrialization, can promote the economic and technological development of osimertinib activeingredients, reduces production cost, and is suitable for mass production.

2,4-dibasic miazines compound

The invention belongs to the field of medical chemistry, relates to a 2,4-dibasic miazines compound and specifically relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof, a drug compound thereof and an application thereof in treating EGFR or/and ALK mediated diseases.

Method for synthesizing 3-amino-4-methoxy acetanilide by binary alloy catalysis

The invention relates to a method for synthesizing 3-amino-4-methoxy acetanilide by catalytically hydrogenising 3-nitro-4-methoxy acetanilide (NMA) with a nano copper/ silver binary alloy catalyst, and belongs to the field of nano catalysis. The reaction

2-amino-4 - (β-hydroxyethyl amino) anisole and its sulphate preparation method

The invention relates to 2-amino-4-(beta-hydroxyethylamino) methoxybenzene and a preparation method of 2-amino-4-(beta-hydroxyethylamino) methoxybenzene sulfate. The preparation method comprises the steps as follows: 3-nitro-para-fluoroaniline is adopted as a raw material and subjected to nucleophilic substitution to produce 3-nitro-4-anisidine; 3-nitro-4-anisidine and chloroethyl chloroformate are subjected to condensation to synthesize 2-nitro-4-(beta-hydroxyethylamino) methoxybenzene with a hydrolysis and decarboxylation one-pot method; and 2-nitro-4-(beta-hydroxyethylamino) methoxybenzene has the hydrogenation reduction reaction to obtain a target product 2-amino-4-(beta-hydroxyethylamino) methoxybenzene which reacts with sulfate salt to obtain 2-amino-4-(beta-hydroxyethylamino) methoxybenzene sulfate. 2-amino-4-(beta-hydroxyethylamino) methoxybenzene and the preparation method of 2-amino-4-(beta-hydroxyethylamino) methoxybenzene sulfate have the advantages of high product quality, good yield, stable technology, small emission of three wastes, low cost, good economic efficiency and the like, and synthesis materials are easy to obtain.

Altering the regioselectivity of a nitroreductase in the synthesis of arylhydroxylamines by structure-based engineering

Nitroreductases have great potential for the highly efficient reduction of aryl nitro compounds to arylhydroxylamines. However, regioselective reduction of the desired nitro group in polynitroarenes is still a challenge. Here, we describe the structure-based engineering of Escherichia coli nitroreductase NfsB to alter its regioselectivity, in order to achieve reduction of a target nitro group. When 2,4-dinitrotoluene was used as the substrate, the wild-type enzyme regioselectively reduced the 4-NO2 group, but the T41L/N71S/F124W mutant primarily reduced the 2-NO2 group, without loss of activity. The crystal structure of T41L/N71S/F124W and docking experiments indicated that the regioselectivity change (from 4-NO2 to 2-NO2) might result from the increased hydrophobicity of residues 41 and 124 (proximal to FMN) and conformational changes in residues 70 and 124. The regioselectivity of nitroreductase NfsB from E. coli toward 2,4-dinitrotoluene was shifted from the 4-NO2 group to the 2-NO2 group without loss of activity, by introducing three mutations: T41L, N71S, and F124W. This study provides an example of a tailored enzyme for regioselective synthesis of the target arylhydroxylamines.

Design, synthesis, and biological evaluation of (E)-N-Aryl-2- arylethenesulfonamide analogues as potent and orally bioavailable microtubule-targeted anticancer agents

A series of novel (E)-N-aryl-2-arylethenesulfonamides (6) were synthesized and evaluated for their anticancer activity. Some of the compounds in this series showed potent cytotoxicity against a wide spectrum of cancer cell-lines (IC50 values ranging from 5 to 10 nM) including all drug resistant cell-lines. Nude mice xenograft assays with compound (E)-N-(3-amino-4- methoxyphenyl)-2-(2′,4′,6′-trimethoxyphenyl)ethenesulfonamide (6t) showed dramatic reduction in tumor size, indicating their in vivo potential as anticancer agents. A preliminary drug development study with compound 6t is predicted to have increased blood-brain barrier permeability relative to many clinically used antimitotic agents. Mechanistic studies indicate that 6t and some other analogues disrupted microtubule formation, formation of mitotic spindles, and arrest of cells in mitotic phase. Compound 6t inhibited purified tubulin polymerization in vitro and in vivo and circumvented drug resistance mediated by P-glycoprotein. Compound 6t specifically competed with colchicine binding to tubulin and with similar avidity as podophylltoxin, indicating its binding site on tubulin.

Functionalized alkoxy arene diazonium salts from paracetamol

Arene diazonium tetrafluoroborates can be synthesized from aromatic acetamides via a sequence of deacetylation, diazotation and precipitation, induced by anion exchange. The reaction is conducted as a convenient one-flask transformation with consecutive addition of the appropriate reagents. Exchange of solvents or removal of byproducts prior to isolation of the product is not required. The arene diazonium salts are isolated from the reaction mixture by simple filtration. Two complementary protocols are presented, and the utility of the reaction is exemplified for a synthesis of the diarylheptanoid natural product de-O-methyl centrolobine.

Efficient and practical cross-coupling of arenediazonium tetrafluoroborate salts with boronic acids catalyzed by palladium(0)/barium carbonate

The cross-coupling reaction of arenediazonium tetrafluoroborate salts with boronic acids catalyzed by the unusual palladium(0)/barium carbonate catalyst is described as an extremely practical and highly efficient alternative to classical homogeneous conditions. Reactions are conducted under mild conditions at room temperature without any base and ligand. The opportunity of preparing unsymmetrical terphenyls in a one-pot process is also demonstrated. Finally, the power of this methodology is highlighted by the synthesis of Bifenazate.