192767-02-5

Upstream product

• 192767-12-7 (3,4-bis-difluoromethoxy-phenyl)-{4-[2,2,2-trifluoro-1-trifluoromethyl-1-(2-trimethylsilanyl-ethoxymethoxy)-ethyl]-phenyl}-methanol 
• 192767-13-8 [2-(1-{4-[(3,4-bis-difluoromethoxy-phenyl)-chloro-methyl]-phenyl}-2,2,2-trifluoro-1-trifluoromethyl-ethoxymethoxy)-ethyl]-trimethyl-silane 
• 192767-03-6 2-(4-bromophenyl)-2-[2-(trimethylsilyl)ethoxymethoxy]-1,1,1,3,3,3-hexafluoropropane 
• 151103-08-1 4-difluoromethoxy-3-hydroxybenzaldehyde 
• 139-85-5 3,4-dihydroxybenzaldehyde 
• 127842-54-0 3,4-bis-(difluoromethoxy)-benzaldehyde 
• 2402-72-4 2-(4-bromophenyl)-1,1,1,3,3,3-hexafluoro-2-propanol 
• 106-37-6 1.4-dibromobenzene 
• 192767-16-1 4-(2-(3,4-bis-difluoromethoxy-phenyl)-2-{4-[2,2,2-trifluoro-1-trifluoromethyl-1-(2-trimethylsilanyl-ethoxymethoxy)-ethyl]-phenyl}-ethyl)-3,5-dichloro-pyridine 

Relevant academic research and scientific papers

Improving metabolic stability of phosphodiesterase-4 inhibitors containing a substituted catechol: Prevention of reactive intermediate formation and covalent binding

A detailed study directed towards metabolic stability optimization of the alkoxy substituents on the catechol moiety of CDP-840 is reported. Replacement of the methoxy and cyclopentyloxy substituents by cyclobutyloxy and/or difluromethoxy groups resulted in the discovery of potent and selective PDE4 inhibitors where the formation of reactive metabolites that could covalently bind to microsomal protein was significantly reduced or eliminated.