142015-63-2

Upstream product

• 1189-71-5 isocyanate de chlorosulfonyle 
• 94-09-7 p-aminoethylbenzoate 

Downstream Products

• 142015-75-6 3-[4-[1-(2-cyano-5-methyl pyrrolyl)]benzyl]-7-methyl-2-propyl-3H-imidazo[4,5-b]pyridine 
• 142015-67-6 1-(4-methanesulfonyloxymethylphenyl)-5-methylpyrrole-2-carbonitrile 
• 142014-44-6 7-Methyl-3-[4-[2-methyl-5-(1H-tetrazol-5-yl)-1-pyrrolyl]benzyl]-2-propyl-3H-imidazo[4,5-b]pyridine 
• 142015-65-4 1-(4-hydroxymethylphenyl)-5-methylpyrrole-2-carbonitrile 
• 142015-80-3 4-chloro-1-(4-ethoxycarbonylphenyl)-5-methylpyrrole-2-carbonitrile 

Relevant academic research and scientific papers

Pilot scale synthesis of a novel nonpeptide angiotensin II receptor antagonist

FR143187 is a novel nonpeptide angiotensin II receptor antagonist under development at Fujisawa Pharmaceutical Co. for the treatment of hypertension. Development of a process for preparation on a large scale is described. The optimized process is 10 steps in length and uses only commercially available materials for each step. Efficient methylation of the 2-position of a pyrrole derivative was achieved by reduction of a Mannich base via the quaternary ammonium salt. Selective cyanation directed by a solvent effect was also investigated. Process improvement efforts focused on optimized reaction conditions for each step, leading to a high-quality product according to a new and concise synthetic route.

ANGIOTENSIN II ANTAGONIZING HETEROCYCLIC DERIVATIVES

The invention relates to compounds of the formula STR1 wherein STR2 represents a condensed or uncondensed imidazolyl ring and the rest of the variables are as defined in the specification. They are angiotensin II antagonists useful for treating hypertension, etc..