55120-56-4

Upstream product

• 52427-05-1 2-bromo-5-nitrophenol 
• 55065-94-6 N-(4-bromo-3-hydroxyphenyl)acetamide 
• 591-27-5 m-Hydroxyaniline 
• 586-11-8 3,5-dinitrophenol 
• 19056-40-7 4-bromo-3-methoxyaniline 
• 121-88-0 5-Nitro-2-aminophenol 
• 860209-11-6 3-amino-2-bromo-5-nitro-phenol 
• 116296-08-3 acetic acid-(3-hydroxy-5-nitro-anilide) 
• 618-64-4 3-Amino-5-nitro-phenol 

Downstream Products

• 6626-15-9 4-Bromoresorcinol 
• 127943-83-3 3-(benzyloxy)-4-bromoaniline 
• 1005786-70-8 N-[6-(5-amino-2-bromophenoxy)imidazo[1,2-b]pyridazin-2-yl]cyclopropanecarboxamide 
• 1584736-31-1 C₉H₁₀BrNO₃ 
• 1584736-34-4 C₁₇H₁₆BrNO₅ 
• 1584736-36-6 C₂₄H₂₃NO₆ 
• 1584736-37-7 C₂₄H₂₃NO₆ 
• 55065-94-6 N-(4-bromo-3-hydroxyphenyl)acetamide 

Relevant academic research and scientific papers

Coumarins by Direct Annulation: β-Borylacrylates as Ambiphilic C3-Synthons

Modular β-borylacrylates have been validated as programmable, ambiphilic C3-synthons in the cascade annulation of 2-halo-phenol derivatives to generate structurally and electronically diverse coumarins. Key to this [3+3] disconnection is the BPin unit which serves a dual purpose as both a traceless linker for C(sp2)–C(sp2) coupling, and as a chromophore extension to enable inversion of the alkene geometry via selective energy transfer catalysis. Mild isomerisation is a pre-condition to access 3-substituted coumarins and provides a handle for divergence. The method is showcased in the synthesis of representative natural products that contain this venerable chemotype. Facile entry into π-expanded estrone derivatives modified at the A-ring is disclosed to demonstrate the potential of the method in bioassay development or in drug repurposing.

SECOND GENERATION INHIBITORS OF MITOCHONDRIAL PERMEABILITY TRANSITION PORE WITH IMPROVED PLASMA STABILITY

The present invention provides compounds useful as mitochondrial permeability transition pore (mtPTP) inhibitors, the compounds being of Formula (I), or a pharmaceutically acceptable salt thereof wherein R11 is selected from the group of H, halogen, and C11-C33 alkyl; and R22 is selected from the group of H, CF33, and halogen; with the proviso that at least one of R11 and R22 is halogen or CF33.

Discovery of meta-amido bromophenols as new antitubercular agents

A series of meta-amido bromophenol derivatives were designed and synthesized. The compounds were found to potently inhibit the growth of Mycobacterium tuberculosis H37Ra. They also exhibited moderate inhibitory activity against Mycobacterium tuberculosis H37Rv and multidrug-resistant strains. The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. Moderate cytotoxicities and good metabolic stability were observed for the selected compounds. The results demonstrated meta-amido bromophenols as a new class of antitubercular agents with good potentials.

Second-Generation Inhibitors of the Mitochondrial Permeability Transition Pore with Improved Plasma Stability

Excessive mitochondrial matrix Ca2+ and oxidative stress leads to the opening of a high-conductance channel of the inner mitochondrial membrane referred to as the mitochondrial permeability transition pore (mtPTP). Because mtPTP opening can lead to cell death under diverse pathophysiological conditions, inhibitors of mtPTP are potential therapeutics for various human diseases. High throughput screening efforts led to the identification of a 3-carboxamide-5-phenol-isoxazole compounds as mtPTP inhibitors. While they showed nanomolar potency against mtPTP, they exhibited poor plasma stability, precluding their use in in vivo studies. Herein, we describe a series of structurally related analogues in which the core isoxazole was replaced with a triazole, which resulted in an improvement in plasma stability. These analogues were readily generated using the copper-catalyzed “click chemistry”. One analogue, N-(5-chloro-2-methylphenyl)-1-(4-fluoro-3-hydroxyphenyl)-1H-1,2,3-triazole-4-carboxamide (TR001), was efficacious in a zebrafish model of muscular dystrophy that results from mtPTP dysfunction whereas the isoxazole isostere had minimal effect.

SUBSTITUTED PYRIDOBENZODIAZEPINONE-DERIVATIVES AND USE THEREOF

The present application relates to novel (3-hydroxyphenyl)amino-substituted pyrido[2,3-b][1,5]benzodiazepin-5-one derivatives, to processes for preparation thereof, to the use thereof alone or in combination for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially of angiogenic disorders and hyperproliferative disorders in which neovascularization plays a role, for example ophthalmological disorders and cancers and tumours. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

DIHYDROQUINOLINONE DERIVATIVES

The present invention relates to new dihydroquinolinone derivatives as defined in formula (I), as well as to a new process for the manufacture of dihydroquinolinone derivatives. The invention further relates to the use of said dihydroquinolinone derivativ

Polymer-anchored peroxo compounds of molybdenum and tungsten as efficient and versatile catalysts for mild oxidative bromination

A polymer supported peroxomolybdate(VI) compound of the type [MoO 2(O2)(CN)2]-PAN [PAN = poly(acrylonitrile)] (PANMo) was obtained by reacting H2MoO4 with 30% H 2O2 and the macromolecular ligand, PAN at near neutral pH. The macrocomplex has been characterized by elemental analysis (CHN and EDX analysis), spectral (IR, UV-Vis and 13C NMR, 95Mo NMR), thermal (TGA-DTG) as well as SEM studies. The catalytic activity of PANMo and its previously reported tungsten containing analog PANW, in oxidative bromination of organic substrates has been explored. The supported complexes could serve as efficient heterogeneous catalysts for the oxidative bromination of a variety of structurally diverse aromatic compounds, with H 2O2 as terminal oxidant, to afford bromo organics in impressive yields under environmentally clean conditions. The catalysts afforded regeneration and could be reused for a minimum of six reaction cycles.

FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF

The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.

Regioselective, photochemical bromination of aromatic compounds using N-bromosuccinimide

Regioselective nuclear bromination of aromatic compounds is investigated with N-bromosuccinimide as the brominating agent under UV irradiation to afford the corresponding brominated compounds. The reaction proceeds at ambient temperature (30 ± 2 °C) without any catalyst. In most of the reactions, regioselectively mono-brominated products are obtained in good to high yields. The conversion and selectivity for bromination depend on the nature of the substituent on the aromatic ring.

Quinoline derivatives

Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.