The invention relates to an intermediate for preparing
azilsartan and a novel preparation method for the
azilsartan. The method includes the following steps: 1) reducing 2-cyano-4'-bromomethylbiphenyl with
hydroxylamine hydrochloride to generate (Z)-4'-bromomethyl-(N')-hydroxy-[1,1'-
biphenyl]-2-
amidine; 2) performing esterification with
ethyl chloroformate to generate (Z)-4'-bromomethyl-(N')-((ethoxycarbonyl)oxyl)-[1,1'-
biphenyl]-2-
amidine; 3) performing ring closing to prepare 3-(4'-(bromomethyl)-[1,1'-
biphenyl]-2-yl)-1,2,4-
oxadiazole-5-(4H)-one; 4) performing a
condensation reaction to 2-ethoxy-1H-
benzimidazole-7-methyl
carboxylate and the 3-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1,2,4-
oxadiazole-5-(4H)-one to prepare 2-ethoxy-1-((2'-(2,5-dihydro-5-oxy-1,2,4-
oxadiazole-3-yl)biphenyl-4-yl)methyl)
benzimidazole-7-methyl
carboxylate; and 5) finally performing
hydrolysis to prepare the
azilsartan. The method employs the
raw material being easy to obtain, is short in synthetic
route, is low in device cost, is less in side products, is low in
toxicity and
pollution, is environment-friendly, is high in product purity and is suitable for industrial production.