150726-86-6

Upstream product

• 6292-59-7 4-tert-butylbenzenesulphonamide 
• 150726-83-3 4,6-dichloro-5-(o-methoxyphenoxy)-2-methyl-pyrimidine 
• 329924-93-8 5-(o-methoxyphenoxy)-4,6-dihydroxy-2-methyl-pyrimidine 
• 20730-58-9 2-(2-Methoxyphenoxy)propanedioic acid diethyl ester 

Downstream Products

• 150726-07-1 p-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(o-methoxy-phenoxy)-2-methyl-4-pyrimidinyl]benzenesulfonamide 

Relevant academic research and scientific papers

6 alkoxy-4-pyrimidinyl bis-sulfonamides

The present invention relates to novel bis-sulfonamides represented, for example, by formula I below and a pure diastereomer, a mixture of diastereomers, a diastereomeric racemate, a mixture of diastereomeric racemates and meso-forms and a pharmaceutically acceptable salt thereof, wherein R1represents aryl; aryl-lower alkyl; aryl-lower alkenyl; heteroaryl; or heteroaryl-lower alkyl; and R2represents lower alkyl; trifluoromethyl; lower alkoxy-lower alkyl; lower alkenyl; lower alkynyl; aryl; aryl-lower alkyl; aryl-lower alkenyl; heterocyclyl; heterocyclyl-lower alkyl; heteroaryl; heteroaryl-lower alkyl; cycloalkyl; or cycloalkyl-lower alkyl. The present invention also relates to a process for manufacturing those compounds, pharmaceutical compositions containing one or more of those compounds as endothelin antagonists, and a method of treating a subject having a disorder involving endothelin with the compounds of the invention.

Modifications and structure-activity relationships at the 2-position of 4-sulfonamidopyrimidine derivatives as potent endothelin antagonists

To improve water solubility and to study structure-activity relationships, we modified the structure of the pyrimidine nucleus of each of a series of potent ETA antagonists, 3a and 4a, at the 2-position. In a previous study, each of these antag