147403-52-9Relevant articles and documents
AZILSARTAN ALKYL ESTER, METHOD FOR PRODUCING AZILSARTAN METHYL ESTER, AND METHOD FOR PRODUCING AZILSARTAN
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Paragraph 0096, (2021/04/17)
PROBLEM TO BE SOLVED: To provide azilsartan alkyl ester to be an intermediate of azilsartan, and a method for producing azilsartan methyl ester having a novel crystal form, and a method for producing high-purity azilsartan from an obtained compound. SOLUTION: The present invention provides a method for producing high-purity azilsartan alkyl ester and/or azilsartan methyl ester by crystallizing azilsartan alkyl ester and/or azilsartan methyl ester in acetone or a solvent mixture of acetone and alcohol. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2021,JPOandINPIT
Synthesis technology for continuously preparing azilsartan in micro-channel reactor
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Paragraph 0053-0059, (2020/02/19)
The invention discloses a synthesis technology for continuously preparing azilsartan in a micro-channel reactor. The technology comprises the following steps: (1) adding SM-1, an aqueous hydroxylaminesolution and triethylamine into anhydrous ethanol, and performing a reaction to obtain an intermediate TAK1; (2) preparing a homogeneous solution A from the TAK1, triethylamine and dioxane; (3) preparing a homogeneous solution B from solid phosgene and dioxane; (4) dissolving sodium hydroxide in water to prepare a homogeneous solution C; (5) respectively pumping the homogeneous solution A and thehomogeneous solution B into a microstructure mixer I in a micro-channel reaction device at the same time, performing mixing, and introducing the obtained mixed solution into a microstructure reactorI; (6) respectively pumping the homogeneous solution C and the effluent of the microstructure reactor I into a microstructure mixer II in the micro-channel reaction device at the same time while step(5) is carried out, performing mixing, and introducing the obtained mixed solution into a microstructure reactor II; and (7) collecting the effluent of the microstructure reactor II to obtain the product azilsartan.
Preparation 2 - ethoxy - 1 - {[2' - (5 - oxo - 4, 5 - dihydro - 1, 2, 4 - oxadiazol - 3 - yl) biphenyl - 4 - yl] methyl} - 1 H - benzimidazole - 7 - carboxylic acid
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, (2018/02/04)
The invention provides a novel method for preparing 2- ethyoxyl-1-{[2'-(5-carbonyl-4,5-dihydro-1,2,4-oxadiazole-3-yl) xenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid. The novel method comprises the steps of providing a novel intermediate in 2-ethyoxyl-1-{[2'-(5-carbonyl-4,5-dihydro-1,2,4-oxadiazole-3-yl)xenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid (azilsartan) preparation, wherein the intermediate is as shown in formula (A); X is H or halogen. By preparing the intermediate with the formula (A), azilsartan can be conveniently and quickly prepared; and moreover, the novel method is short in reaction route, less in byproduct, high in total yield, gentle in condition and suitable for industrially preparing azilsartan.