CAJ | 학술논문

目的合成抗高血压新药奥美沙坦的关键中间体2-丙基-1H-咪唑-4,5-二羧酸二乙酯. 方法以价廉易得、可再生的酒石酸为起始原料,经混酸硝化后与醛氨溶液缩合,再经酯化制得.结果取代了文献中有毒的原料,改进了合成工艺,总收率提高到70%.结论以酒石酸为起始原料的改进后的合成方法收率提高,反应条件温和,适合工业化生产.
목적 합성항고혈압신약오미사탄적관건중간체2-병기-1H-미서-4,5-이최산이을지. 방법이개렴역득、가재생적주석산위기시원료,경혼산초화후여철안용액축합,재경지화제득.결과 취대료문헌중유독적원료,개진료합성공예,총수솔제고도70%.결론 이주석산위기시원료적개진후적합성방법수솔제고,반응조건온화,괄합공업화생산.
Objective To synthesize the important intermediates of Olmesartan.Methods 2-propyl-1H-imidazole-4,5-dicarboxylic acid diethyl ester was synthesized using tartaric acid,an easily available,inexpensive and renewable substrate,as starting material via nitration,cyclization,esterifcation.Results The technics was improved and toxic material was replaced.The overall yield was 70%.Conclusion The improved method is of high yield,more practical,facile and suitable for industry.