58022-58-5

Upstream product

• 177755-73-6 2-hydroxy-2-(4-methylthiophenyl)-1-phenylethanone 
• 73242-07-6 2-phenyl-4'-(methylthio)acetophenone 
• 103-80-0 phenylacetyl chloride 
• 100-68-5 methyl-phenyl-thioether 
• 532-28-5 (RS)-mandelonitrile 
• 1074-12-0 phenylglyoxal hydrate 
• 177755-47-4 1-(3-fluoro-4-methoxyphenyl)-2-[4-(methylthio)phenyl]ethane-1,2-dione 
• 63571-96-0 S-ethyl 2-oxo-2-phenylethanethioate 
• 3446-89-7 4-(Methylthio)benzaldehyde 
• 95392-03-3 2-(3,4-dichlorophenyl)-2-((trimethylsilyl)oxy)acetonitrile 
• 177755-55-4 1-(3,4-dichlorophenyl)-2-hydroxy-2-[4-(methylthio)phenyl]ethanone 

Downstream Products

• 146857-52-5 4-methylmercaptobenzilic acid 
• 177755-74-7 4-[4-(methylthio)phenyl]-5-phenyl-2-(trifluoromethyl)-1H-imidazole 
• 54945-18-5 1-(4-methanesulfonyl-phenyl)-2-phenyl-ethane-1,2-dione 
• 146857-54-7 4-methylmercaptodiphenylacetic acid 
• 146857-53-6 4-methylsulfonylbenzilic acid 
• 177560-74-6 1-phenyl-2-[4-(methylthio)phenyl]-ethan-1-one 
• 1616468-91-7 3-methylthio-5-(4-methylthiophenyl)-6-phenyl-1,2,4-triazine 
• 1616468-92-8 3-methylthio-5-phenyl-6-(4-methylthiophenyl)-1,2,4-triazine 
• 699003-41-3 5-(4-methylsulfonylphenyl)-6-phenyl-2,3-dihydropyrazine 

Relevant academic research and scientific papers

1,2-dicarbonyl compound and synthesis method thereof

The invention discloses a method for synthesizing a 1,2-dicarbonyl compound (1,2-dicarbonylamide or alpha-diketone compound), wherein 1,2-dicarbonyl thioester compounds used as 1,2-dicarbonyl reagentsreact with amine compounds or boric anhydride compounds under appropriate conditions to respectively synthesize a series of 1,2-dicarbonyl compounds. According to the present invention, the 1,2-dicarbonyl compound is obtained by using the stable 1,2-dicarbonyl thioester compound as the dicarbonylation reagent through one-step construction under mild conditions, such that the disadvantage that thetraditional method uses the unstable alpha-carbonyl acyl chloride to synthesize the 1,2-dicarbonyl compound is avoided.

Synthesis, antileukemic and antiplatelet activities of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines

The synthesis, antileukemic and antiplatelet activity evaluation of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines are described. In general, it was found that compound 17o showed moderate antileukemic activity against MOLT3 human leukemic cancer cell lines. An arachidonic acid induced platelet aggregation effect on washed rat platelets was studied. Compound 17i was found to be the most potent. The antiplatelet properties may be mediated by interference with the arachidonic acid pathway.

Synthesis of novel substituted diaryl-1,4-diazepines

In this paper a convenient route to new 2,3-diaryl-substituted 1,4-diazepines is described through cyclization of ethanedione derivatives and 1,3-propanediamine. The ethanedione derivatives required were synthesized by microwave-assisted oxidation from ethanones.

Synthesis and biological evaluation of 2,3-diarylpyrazines and quinoxalines as selective COX-2 inhibitors

Several 2,3-diaryl pyrazines and quinoxalines with 4-sulfamoyl (SO 2NH2)/methylsulfonyl (SO2Me)-phenyl pharmacophores have been synthesized and evaluated for the cyclooxygenase (COX-1/COX-2) inhibitory activity. Smaller groups such as methoxy, methyl and fluoro when substituted at/around position-4 of the adjacent phenyl ring, have great impact on the selective COX-2 inhibitory activity of the series. Many potential compounds were obtained from a brief structure-activity relationship (SAR) study. Two of these, compounds 11 and 25 exhibited excellent in vivo activity in the established animal model of inflammation. Since compound 25 possessed an amenable sulfonamide group, two of its prodrugs 48 and 49 were also synthesized. Both of them have excellent in vivo potential, and represent a new class of COX-2 inhibitor.

Antiinflammatory 4,5-diarylimidazoles as selective cyclooxygenase inhibitors

The synthesis and activity of a series of 4,5-diarylimidazole analogs are described. One analog had an IC50 of 80 nM, was 6750-selective against COX-1, and demonstrated in vivo potency in the mouse air pouch model.

Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation

A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II STR1 wherein R1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower aralkenyl, lower aryloxyalkyl, lower arylthioalkyl and heteroaryl; wherein R3 is selected from lower alkyl and amino; and wherein R4 is one or more radicals selected from hydrido, halo, lower alkyl and lower alkoxy; or where R4 together with the phenyl radical forms naphthyl or benzodioxolyl; provided R1 is not lower alkyl when R3 is methyl and when R4 is hydrido, methyl, methoxy or chloro; or a pharmaceutically-acceptable salt thereof.