344457-87-0

Upstream product

• 452-71-1 4-fluor-2-methylaniline 
• 740815-24-1 (4-bromo-2-chlorophenyl)(2-methylphenyl)methanone 
• 31928-47-9 4-bromo-2-chloroiodobenzene 
• 529-20-4 2-methylphenyl aldehyde 
• 740815-23-0 (4-bromo-2-chlorophenyl)(2-methylphenyl)methanol 
• 344459-21-8 (2-chloro-4-nitrophenyl)(2-methylphenyl)methanone 
• 7073-36-1 2-chloro-4-nitrobenzoyl chloride 
• 99-60-5 2-chloro-4-nitrobenzoic acid 

Downstream Products

• 720685-83-6 [3-chloro-4-(2-methyl-benzoyl)-phenyl]-(4-fluoro-2-methyl-phenyl)-carbamic acid 1-chloro-ethyl ester 
• 344458-06-6 2-Chloro-4-(4-fluoro-2-methyl-N-methyl-phenylamino)-2'-methylbenzophenone 
• 720685-89-2 [3-chloro-4-(2-methyl-benzoyl)-phenyl]-(4-fluoro-2-methyl-phenyl)-carbamic acid chloromethyl ester 

Relevant academic research and scientific papers

Rapid and efficient microwave-assisted synthesis of aryl aminobenzophenones using Pd-catalyzed amination

Substituted aryl aminobenzophenone p38 MAP kinase inhibitors were synthesized in good to excellent yields using palladium-catalyzed aryl amination under conditions of microwave irradiation. Various ligands have been screened, and the reaction conditions w

Synthesis and Structure-Activity Relationship of Aminobenzophenones. A Novel Class of p38 MAP Kinase Inhibitors with High Antiinflammatory Activity

We wish to report the synthesis and structure-activity relationship (SAR) of a series of 4-aminobenzophenones, as a novel compound class with high antiinflammatory activity. Our initial lead, {4-[(2-aminophenyl)amino]phenyl}(phenyl)methanone (3), was systematically optimized and resulted in compounds that potently inhibited the release of the proinflammatory cytokines IL-1β and TNF-α in human peripheral blood mononuclear cells stimulated by LPS. One of the most potent compounds, among others, was {4-[(2-aminophenyl)amino]-2-chlorophenyl}(2-methylphenyl)methanone (45) with IC50 values of 14 and 6 nM for the inhibition of IL-1β and TNF-α, respectively. Furthermore, we found these types of compounds to be potent and selective p38 MAP kinase inhibitors, e.g. 45 had an IC50 value of 10 nM. Molecular modeling was used to rationalize our SAR data and to propose a model for the interaction of compound 45 with the p38 MAP kinase. The model involved a favorable hydrogen bond between the carbonyl group of the benzophenone and the NH of Met-109, positioning ring A in the hydrophobic pocket I of the enzyme. Good antiinflammatory effects were demonstrated in two murine models of dermatitis after topical application (oxazolone and TPA model).

Dermal anti-inflammatory composition

A pharmaceutical composition for dermal application comprises a lipophilic anti-inflammatory compound and a pharmaceutically acceptable vehicle comprising a lipophilic excipient capable of solubilizing the anti-inflammatory compound and targeting said compound to the pilosebaceous ducts on application of the composition on the skin. The composition may be used in the treatment of dermal inflammatory conditions, in particular acne.