18920-70-2

Usage

Preparation

Obtained by Fries rearrangement of phenyl p-nitro-benzoate with aluminium chloride, ? without solvent at 140° for 30 min (52%), at 120° for 2 h (21%) or first at 130° for 1 h, then at 160° for 1 h (2%); ? in refluxing chlorobenzene for 5 h (24%).

Upstream product

• 1429-05-6 phenyl 4-nitrobenzoate 
• 69557-75-1 4-ethoxy-4'-nitro-benzophenone 
• 122-04-3 4-nitro-benzoyl chloride 
• 100-66-3 methoxybenzene 
• 103-73-1 Phenetole 
• 1151-94-6 4-methoxy-4'-nitrobenzophenone 
• 25458-45-1 p-methoxymethoxybromobenzene 
• 106-41-2 4-bromo-phenol 

Downstream Products

• 83355-03-7 <4-(4-nitrobenzoyl)phenyl>-2,3,4-tri-O-acetyl-β-D-xylopyranoside 
• 1151-94-6 4-methoxy-4'-nitrobenzophenone 
• 835889-67-3 4-(2-hydroxyethoxy)-4'-nitrobenzophenone 
• 69557-75-1 4-ethoxy-4'-nitro-benzophenone 
• 221532-00-9 4-(4-isopropoxybenzoyl)-nitrobenzene 

Relevant academic research and scientific papers

Liquid-Phase Total Synthesis of Plecanatide Aided by Diphenylphosphinyloxyl Diphenyl Ketone (DDK) Derivatives

Plecanatide is an oral guanylate cyclase-C agonist for the treatment of gastrointestinal disorders. The large-scale supply of plecanatide is restrained primarily by its industrial manufacture. Herein we developed diphenylphosphinyloxyl diphenyl ketone (DD

Inducing apoptosis through upregulation of p53: structure–activity exploration of anthraquinone analogs

We previously reported a series of p53-elevating anthraquinone compounds with considerable cytotoxicity for acute lymphoblastic leukemia (ALL) cells. To further develop this class of compounds, we examined the effect of a few key structural features on the anticancer structure–activity relationship (SAR) in ALL cells. The active analogs showed comparable cytotoxicity and upregulation of p53 but did not induce significant downregulation of MDM2 as seen with the lead compound AQ-101, indicating the importance of the anthraquinone core scaffold for MDM2 regulation. The result from the current study not only contributes to the SAR framework of these anthraquinone derivatives but also opens up new chemical space for further optimization work.

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I): wherein,R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable s

PHOTOACTIVATABLE FOULING-RESISTANT COPOLYMERS

A photoactivatable fouling-resistant copolymer composed of a photoactivatable monomer and a hydrophilic monomer is disclosed. The photoactivatable monomer includes an aryl ketone derivative having one or more polar groups or alkyl groups.

Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities

Both selective estrogen receptor modulators and aromatase inhibitors are widely used for the treatment of breast cancer. Compounds with both aromatase inhibitory and estrogen receptor modulatory activities could have special advantages for treatment of br

Radiosynthesis and evaluation of an 18F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype

A known chemotype of H3 receptor ligand was explored for development of a radioligand for imaging brain histamine subtype 3 (H 3) receptors in vivo with positron emission tomography (PET), namely nonimidazole 2-aminoethylbenzofurans,

Synthesis and characterization of fluorinated polyimides derived from novel unsymmetrical diamines

Two kinds of aromatic, unsymmetrical diamines with ether-ketone group, 3-amino-4'-(4-amino-2- trifluoromethylphenoxy)-benzophenone and 4-amino-4'-(4-amino-2-trifluoromethylphenoxy)-benzophenone, were successfully synthesized with two different synthetic r

Optimised synthesis and photochemistry of antenna-sensitised 1-acyl-7-nitroindolines

Benzophenone antenna-sensitised 1-acyl-7-nitroindolines show a significantly enhanced extent of photochemical cleavage in aqueous solution over their non-sensitised analogues and release the carboxylate derived from their 1-acyl group. The present work in

Discovery and SAR development of 2-(phenylamino) imidazolines as postacyclin receptor antagonists

On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d [(4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxybenzyl)phenyl] amine] had analgesic activity in the rat.

Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors

New orally active non-terpenoic inhibitors of human 2,3-oxidosqualene cyclase (hOSC) are reported. The starting point for the optimization process was a set of compounds derived from a fungicide project, which in addition to showing high affinity for OSC from Candida albicans showed also high affinity for human OSC. Common structural elements of these inhibitors are an amine residue and an electrophilic carbonyl C atom embedded in a benzophenone system, which are at a distance of about 10.7 ?. Considering that the keto moiety is in a potentially labile position, modifications of the substitution pattern at the benzophenone as well as annelated heteroaryl systems were explored. Our approach combined testing of the compounds first for increased binding affinity and for increased stability in vitro. Most promising compounds were then evaluated for their efficacy in lowering plasma total cholesterol (TC) and plasma low-density lipoprotein cholesterol (LDL-C) in hyperlipidemic hamsters. In this respect, the most promising compounds are the benzophenone derivative 1·fumarate and the benzo[d]-isothiazol 24·fumarate, which lowered TC by 40% and 33%, respectively.