NOVEL INTERMEDIATE COMPOUNDS FOR EFFICIENT SYNTHESIS OF VALSARTAN

摘要

PURPOSE: A novel intermediate compound for preparing valsartan and method for preparing valsartan using the same are provided to improve safety and shorten reaction time. CONSTITUTION: A method for preparing valsartan of chemical formula 1 comprises: a step of reacting 4-toluene-2'-(tetrazole-5-yl)-benzene of chemical formula 2 and ethylvinylether under the presence of acid to prepare 4-bromomethyl-2'-(1-diethylether-tetrazole-5-yl)-biphenyl; and a step of binding L-valinemethylester hydrochloride of chemical formula 4 with 4-bromomethyl-2'-(1-diethylether-tetrazole-5-yl)-biphenyl of chemical formula 3 to obtain (S)-3-methyl-2-(2'-(1-diethylether-tetrazole-5-yl)-biphenyl-4-yl-methyl)-butylic acid methyl ester of chemical formula 5; a step of performing N-alkylation of a compound of chemical formula 5 with valeryl chloride of chemical formula 6 to obtain (S)-3-methyl-2'-[N-pentanoyl-(1-diethylether-tetrazole-5-yl)-biphenyl-4-yl-methyl]-amino butylic acid methyl ester; and a step of hydrolyzing the compound of chemical formula 7.