172875-70-6Relevant articles and documents
Preparation method of high-purity triphenyl olmesartan ethyl ester
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Paragraph 0103-0113, (2019/11/25)
The invention provides a preparation method of a high-purity olmesartan medoxomil intermediate triphenyl olmesartan ethyl ester. The provided preparation method specifically comprises the steps that in a first solvent, in the presence of a combined catalyst and potassium carbonate, a compound shown in a formula 2 and a compound shown in a formula 3 react with each other to obtain a compound shownin a formula 1, wherein the combined catalyst is composed of polyethylene glycol and 2-methylpyrrolidone. The preparation method can significantly reduce the content of the impurities shown in a formula 4 and formula 5 in the product intermediate shown in the formula 1, and improve the purity of the intermediate shown in the formula 1.
Nonpeptide angiotensin II receptor antagonists: Synthesis, biological activities, and structure - Activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds
Yanagisawa, Hiroaki,Amemiya, Yoshiya,Kanazaki, Takuro,Shimoji, Yasuo,Fujimoto, Koichi,Kitahara, Yoshiko,Sada, Toshio,Mizuno, Makoto,Ikeda, Masahiro,Miyamoto, Shuichi,Furukawa, Youji,Koike, Hiroyuki
, p. 323 - 338 (2007/10/03)
A series of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds were prepared and evaluated for their antagonistic activities to the angiotensin II (AII) receptor. Among them, the 4-(1-hydroxyalkyl)-imidazole derivatives had strong binding affinity to the AII receptor and potently inhibited the AII-induced pressor response by intravenous administration. Various esters of these acids showed potent and long-lasting antagonistic activity by oral administration. The most promising compounds were (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (CS-866) and (pivaloyloxy)-methyl esters of 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[(2′-1H-tetrazol-5-ylbiphenyl-4-yl) -methyl]imidazole-5-carboxylic acid (26c). A study involving stereochemical comparison of 26c with the acetylated C-terminal pentapeptide of AII was also undertaken.