578727-01-2

Upstream product

• 87022-42-2 1-(isocyanomethyl)-1H-benzo[d][1,2,3]triazole 
• 352-34-1 4-fluoro-1-iodobenzene 
• 190198-32-4 1-(4-methylsulfanylphenyl)-1H-imidazole 
• 104-96-1 4-methylsulfanylaniline 
• 459-57-4 4-fluorobenzaldehyde 
• 104-95-0 (4-bromophenyl)thioanisole 

Downstream Products

• 578727-02-3 5-(4-fluoro-phenyl)-2-methyl-1-(4-methylsulfanyl-phenyl)-1H-imidazole 
• 265113-46-0 5-(4-fluorophenyl)-1-(4-methylsulfonylphenyl)imidazole 

Relevant academic research and scientific papers

Regioselective synthesis of 1,5-diaryl-1H-imidazoles by palladium-catalyzed direct arylation of 1-aryl-1H-imidazoles

A variety of 1,5-diaryl-1H-imidazoles have been regioselectively synthesized by direct coupling of 1-aryl-1H-imidazoles with aryl iodides or bromides in DMF in the presence of CsF as the base and a catalyst precursor consisting of a mixture of Pd(OAc)sub

Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-Diarylimidazoles

The synthesis and the pharmacological activity of a series of 1,5-diarylimidazoles developed as potent and selective cyclooxygenase-2 (COX-2) inhibitors are described. The new compounds were evaluated both in vitro (COX-1 and COX-2 inhibition in human whole blood) and in vivo (carrageenan-induced paw edema, air-pouch, and hyperalgesia tests). Modification of all the positions of two regioisomeric imidazole cores led to the identification of 4-[4-chloro-5-(3-fluoro4-methoxyphenyl)imidazol-1-yl]benzenesulfonamide (UR-8880, 51f) as the best candidate, which is now undergoing Phase I clinical trials.