文献类型：专利

英文题名：Preparing 5-carboxylic acid losartan, comprises taking and reacting 2-butyl-4-chlorine-5-formyl radical-1-(2'-2(1H-tetrazole-5-radical)-biphenyl-4)-methylimidazole as raw material to obtain 5-carboxylic acid losartan by oxidation

作者：WEI Q;WU F;YE W;ZHAO M

机构：[1]UNIV EAST CHINA SCI&TECHNOLOGY

申请号：CN102558156-A

申请日：2012-02-24

公开日：2012-07-11

语种：英文

收录：DERWENT

摘要：NOVELTY - The method comprises taking and reacting 2-butyl-4-chlorine-5-formyl radical-1-((2'-2(1H-tetrazole-5-radical)-biphenyl-4)-methyl) imidazole as raw material for 10 hours to obtain 5-carboxylic acid losartan by oxidation. The reaction temperature is -5 degrees C to 15 degrees C. The method further comprises taking isopropanol as solvent, selecting the mixed solution of hydrogen peroxide and sodium chlorite as oxidizing agent, and deprotecting 2-butyl-4-chlorine-5-formyl radical-1-((2'-2(1-H-tetrazole-5-radical)-biphenyl-4)-methyl) imidazole. USE - The method is useful for preparing 5-carboxylic acid losartan, which is useful for treating hyperlipidemia and hypertension. ADVANTAGE - The method is capable of economically preparing the 5-carboxylic acid losartan with high purity and yield. DETAILED DESCRIPTION - The method comprises taking and reacting 2-butyl-4-chlorine-5-formyl radical-1-((2'-2(1H-tetrazole-5-radical)-biphenyl-4)-methyl) imidazole as raw material for 10 hours to obtain 5-carboxylic acid losartan by oxidation. The reaction temperature is -5 degrees C to 15 degrees C. The method further comprises taking isopropanol as solvent, selecting the mixed solution of hydrogen peroxide and sodium chlorite as oxidizing agent, and deprotecting 2-butyl-4-chlorine-5-formyl radical-1-((2'-2(1-H-tetrazole-5-radical)-biphenyl-4)-methyl) imidazole of the 2-butyl-4-chlorine-5-formyl radical-1-((1'-2(1- trityl-tetranitrogen imidazolyl-5-)-biphenyl-4-)-methyl) imidazole using hydrochloric acid solution at 50 degrees C for 5 hours. A mol ratio of the sodium chlorite and raw material is 1.5:1. The optimal reaction temperature is 5-10 degrees C. A mol ratio of hydrochloric acid and raw material is 2.4:1.