![](/CAS/GIF/147403-03-0.gif)
Azilsartan synthesis
- Product Name:Azilsartan
- CAS Number:147403-03-0
- Molecular formula:C25H20N4O5
- Molecular Weight:456.45
![](https://www.chemicalbook.com/NewsImg/2021-02-09/20210209740008881457918095.jpg)
![QQ截图20210210111404.jpg QQ截图20210210111404.jpg](/NewsImg/2021-02-10/6374855259568279847974619.jpg)
An improved scalable route (Scheme below) to azilsartan was reported and features reproducibly better yields.43 Hydroxyamidine 30 was treated with dimethyl carbonate and sodium methoxide, which triggered they key cyclization along with concomitant transesterification to deliver 29. Milder aqueous sodium hydroxide hydrolysis converted this methyl ester 29 to azilsartan (V) in 88-90% yield.
![1H-BenziMidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]Methyl] -2-ethoxy-, ethyl ester](/CAS/GIF/1403474-70-3.gif)
1403474-70-3
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![Azilsartan](/CAS/GIF/147403-03-0.gif)
147403-03-0
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Yield:147403-03-0 98.5%
Reaction Conditions:
with water;sodium hydroxide at 50; for 4 h;
Steps:
9 Example 9: Preparation of 2-ethoxy-l-((2'-(5-oxo-455-dihydro-l ,2,4-oxadiazol-3-yl)biphenyl- 4-yl)methyl)-lH-benzo[ ]-imidazole-7-carboxylic acid (III).
The starting ethyl ester of azilsartan (V, 250 g) was suspended in a solution of sodium hydroxide in water (56 g/800ml). The suspension was heated at 50°C for 4 h, after pH adjustment to 4-5, the product crystallized providing 232 g (98.5 %).
References:
WO2014/48404,2014,A1 Location in patent:Page/Page column 11
![(Z)-Methyl 2-ethoxy-3-((2'-(N'-(ethoxycarbonyloxy)carbaMiMidoyl)biphenyl-4-yl)Methyl)-3H-benzo[d]iMidazole-4-carboxylate](/CAS/20150408/GIF/147404-82-8.gif)
147404-82-8
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![Azilsartan](/CAS/GIF/147403-03-0.gif)
147403-03-0
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![(Z)-Ethyl-2-ethoxy-3-((2'-(N'-hydroxycarbaMiMidoyl) biphenyl-4-yl) Methyl)-3H-benzo[d] iMidazole-4-carboxylate](/CAS/GIF/1397836-41-7.gif)
1397836-41-7
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![Ethyl chloroformate](/CAS/GIF/541-41-3.gif)
541-41-3
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![Azilsartan](/CAS/GIF/147403-03-0.gif)
147403-03-0
507 suppliers
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![1H-BenziMidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]Methyl] -2-ethoxy-, Methyl ester](/CAS/GIF/147403-52-9.gif)
147403-52-9
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147403-03-0
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![1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2'-[imino[[(phenoxycarbonyl)oxy]amino]methyl][1,1'-biphenyl]-4-yl]methyl]-, methyl ester](/CAS/20210111/GIF/1403477-44-0.gif)
1403477-44-0
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![Azilsartan](/CAS/GIF/147403-03-0.gif)
147403-03-0
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$5.00/50mg