ChemicalBook CAS DataBase List Fimasartan

Fimasartan synthesis

10synthesis methods

Product Name:Fimasartan
CAS Number:247257-48-3
Molecular formula:C27H31N7OS
Molecular Weight:501.65

1361024-52-3 Synthesis

2-(2-butyl-4-Methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)Methyl)-1,6-dihydropyriMidin-5-yl)-N,N-diMethylethanethioaMide

1361024-52-3
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247257-48-3
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Yield:247257-48-3 92%

Reaction Conditions:

with acetic acid in tetrahydrofuran;water; for 2 h;Reflux;

Steps:

6 Example Fimasartan(2-butyl-5-dimethylaminothioformylmethyl)-6-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]Pyrimidine-4(3H)-one)Synthesis

In a 500 mL three-necked flask equipped with a reflux condenser,The intermediate IV synthesized in Example 5 was added to 37.2 g (0.05 mol) and 100 mL of tetrahydrofuran.After stirring and stirring, 25 mL of glacial acetic acid and 6 mL of distilled water were added, and the reaction was refluxed for 2 h;Then neutralize the reaction solution with 4N NaOH solution.The aqueous phase was dried over solid NaCl and extracted three times with ethyl acetate.The organic phase was washed with brine, and the combined organic layer and ethyl acetateAdd the same volume of distilled water and stir for 1 hour, and filter the precipitated solid.Use 50mL of distilled water,Wash with 50 mL of ethyl acetate and 150 mL of isopropyl ether, and dry at 60 ° C for 24 h.23.0 g of Fimasartanwas obtained, and the yield was 92%.

References:

CN109096261,2018,A Location in patent:Paragraph 0052; 0053

503155-67-7 Synthesis