阿曲生坦关键中间体的合成研究  

Synthesis of Key Intermediates of Atrasentan

作　　者：张立颖[1] 刘旭亮[2] 石军 Zhang Liying;Liu Xuliang;Shi Jun(Shandong University of Technology,Zibo 255049,China;Shandong Xinhua Pharmaceutical Co.,Ltd.,Zibo 255086,China)

机构地区：[1]山东理工大学,山东淄博255049 [2]山东新华制药股份有限公司,山东淄博255086

出　　处：《山东化工》2019年第23期42-42,47,共2页Shandong Chemical Industry

摘　　要：以胡椒醛为起始原料,经硝化、还原和拆分制得阿曲生坦关键中间体(2R,3R,4S)-4-(1,3-苯并二氧戊环-5-基)-2-(4-甲氧基苯基)吡咯烷-3-羧酸乙酯,再与2-溴-N,N-二正丁基乙酰胺缩合制得阿曲生坦,纯度大于98.5%。Starting with piperonal,the atrasentan's key intermediate of 3-Pyrrolidinecarboxylic acid,4-(1,3-benzodioxol-5-yl)-2-(4-methoxyphenyl)-,ethyl ester,(2R,3R,4S)-was obtained by nitration,reduction and resolution,and then condensed with 2-bromo-N,N-di-n-butylacetamide to obtain atrasentan with a purity greater than 98.5%.

关 键 词：阿曲生坦 中间体 合成 

分 类 号：TQ463[化学工程—制药化工]