15948-51-3

Upstream product

• 104-88-1 4-chlorobenzaldehyde 
• 3757-16-2 1-(4-nitrostyryl)-4-chlorobenzene 
• 14064-55-2 (E)-4-chloro-4'-nitrostilbene 
• 2609-49-6 diethyl p-nitrobenzylphosphonate 

Downstream Products

• 15851-77-1 {4-[(4-chlorophenyl)ethynyl]phenyl}amine 
• 14064-70-1 (Z)-(4-chlorophenyl)(4'-nitrophenyl)ethene 
• 168151-97-1 N-[4-(4-Chloro-phenylethynyl)-phenyl]-2-cyano-acetamide 
• 168151-99-3 (Z)-(4-aminophenyl)(4'-chlorophenyl)ethene 
• 168151-98-2 N-{4-[(Z)-2-(4-Chloro-phenyl)-vinyl]-phenyl}-2-cyano-acetamide 
• 15852-01-4 1-chloro-4-[(4-nitrophenyl)ethynyl]benzene 

Relevant academic research and scientific papers

Solvolytic stereoselective debromination of vic-dibromides with HMPA

A simple and efficient procedure for the debromination of vic-dibromides has been reported with hexamethylphosphoric triamide at 155-160°C under a nitrogen atmosphere without the aid of any reagent.

Synthesis, structure-activity relationships, and pharmacokinetic properties of dihydroorotate dehydrogenase inhibitors: 2-cyano-3-cyclopropyl- 3-hydroxy. N-[3'-methyl-4'-(trifluoromethyl)phenyl]propenamide and related compounds

The active metabolite (2) of the novel immunosuppressive agent leflunomide (1) has been shown to inhibit the enzyme dihydroorotate dehydrogenase (DHODH). This enzyme catalyzes the fourth step in de novo pyrimidine biosynthesis. A series of analogues of the active metabolite 2 have been synthesized. Their in vivo biological activity determined in rat and mouse delayed type hypersensitivity has been found to correlate well with their in vitro DHODH potency. The most promising compound (3) has shown activity in rat and mouse collagen (II)-induced arthritis models (ED50 = 2 and 31 mg/kg, respectively) and has shown a shorter half-life in man when compared with leflunomide. Clinical studies in rheumatoid arthritis are in progress.