954221-91-1

Upstream product

• 1193-21-1 4,6-dichloropyrimidine 
• 171364-83-3 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)nitrobenzene 
• 586-78-7 para-nitrophenyl bromide 

Downstream Products

• 1376770-23-8 1-(3-(trifluoromethyl)phenyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)urea 
• 1376770-24-9 1-(4-cyanophenyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)urea 
• 1376770-25-0 1-(2-(trifluoromethyl)phenyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)thiourea 
• 1376770-26-1 1-(3-cyanophenyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)thiourea 
• 1376770-27-2 1-(4-methoxyphenyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)thiourea 
• 1376770-28-3 1-(4-chlorophenyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)thiourea 
• 1376770-29-4 1-(2-fluorophenyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)thiourea 
• 1376770-30-7 1-(o-tolyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)thiourea 
• 1376770-31-8 1-(3,5-bis(trifluoromethyl)phenyl)-3-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)thiourea 
• 1376770-32-9 4-bromo-N-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)benzenesulfonamide 
• 1376770-33-0 5-fluoro-2-methyl-N-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)benzenesulfonamide 
• 1376770-34-1 3-methyl-N-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)benzenesulfonamide 
• 1376770-35-2 4-(trifluoromethoxy)-N-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)benzenesulfonamide 
• 1376770-36-3 3-cyano-N-(4-(6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)phenyl)benzenesulfonamide 

Relevant academic research and scientific papers

Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors

As non-receptor tyrosine kinases, Janus kinases (JAKs) have become an attractive target for the treatment of autoimmune diseases and cancers. JAKs play a pivotal role in innate immunity, inflammation, and hematopoiesis by mediating the signaling of numerous cytokines, growth factors, and interferons (IFNs). Selective inhibitors of a variety of JAK members are expected to inhibit pro-inflammatory cytokine-mediated inflammation and immune responses, while preventing targeting other subtypes of JAKs. In this work, poorly selective compounds based on 4- or 6-phenyl-pyrimidine derivatives have been improved to highly potent and selective compounds by designing a covalent binding tether, which attaches to the unique cysteine (Cys909) residue in JAK3. Compound 12 exhibited potent JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile when compared to the other JAK isoforms (>588-fold). In a cellular assay, compound 12 strongly inhibited JAK3-dependent signaling and T cell proliferation. Moreover, in vivo data revealed that compound 12 significantly suppressed oxazolone (OXZ)-induced delayed hypersensitivity responses in Balb/c mice. Compound 12 also displayed decent pharmacokinetic properties and was suitable for in vivo use. Taken together, these results indicated that compound 12 may be a promising tool compound as a selective JAK3 inhibitor for treating autoimmune diseases.

A novel pyrimidine derivatives with aryl urea, thiourea and sulfonamide moieties: Synthesis, anti-inflammatory and antimicrobial evaluation

A series of novel 4-(3-(trifluoromethyl)phenylamino-6-(4-(3-arylureiodo/ arylthioureido/arylsulfonamido)-pyrimidine derivatives of biological interest were prepared by the sequential Suzuki cross coupling, acid amination, reduction followed by reaction of