One kind of azilsartan industrial production method

2013 
The present invention provides a azilsartan industrial production, the method comprising the steps of: 1) hydroxylamine hydrochloride with an organic or inorganic base in a polar aprotic substitutions solvent and centrifuged to a homogeneous system, the Jia Rukan losartan C6 alkyl ester (compound of formula IV), the reaction temperature 90 ~ 110 ℃, a compound of formula III; 2) the compound of formula III with a carbonylating agent dissolved in a polar aprotic solvent, or an organic base is added inorganic bases, 0 ~ 40 ℃ reaction, to give a compound of formulas II, then by alkaline hydrolysis to give azilsartan. The method of preparation of the present invention greatly reduces the manufacturing cost azilsartan, avoiding the use of expensive and unstable hydroxylamine solution, the reaction temperature is lowered, so that product quality has been improved to better achieve a pharmaceutically acceptable level requirements, single hetero all controlled below 0.1%, better than the EU ICH requirements.
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