142014-85-5Relevant academic research and scientific papers
Pilot scale synthesis of a novel nonpeptide angiotensin II receptor antagonist
Zanka, Atsuhiko,Nishiwaki, Masanori,Morinaga, Yasuhiro,Inoue, Takayuki
, p. 230 - 237 (1998)
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
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, (2008/06/13)
The invention concerns compounds of the formula STR1 represents a condensed or uncondensed imidazolyl ring and the rest of the variables are defined in the specification. They are angiotensin II antagonists useful for treating hypertension, etc.
ANGIOTENSIN II ANTAGONIZING HETEROCYCLIC DERIVATIVES
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, (2008/06/13)
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..
