摘要
富马酸比索洛尔为选择性β1-肾上腺素能受体阻滞剂,介绍了一种不对称合成S-富马酸比索洛尔和R-富马酸比索洛尔的新方法。以R-环氧氯丙烷和S-环氧氯丙烷为手性原料,直接与4-((2-异丙氧基乙氧基)甲基)-苯酚缩合,再经开环得到化合物S-比索洛尔和R-比索洛尔,最后与富马酸成盐制得S-富马酸比索洛尔和R-富马酸比索洛尔。
The asymmetric synthesis of S-and R-bisoprolol fumarate, a selective β1-blocker inhibitor with extensive clinical use, is presented in this paper. Firstly R-and S-epichlorohydrin is used as chiral reagent to directly react with 4-（（2-isoproxyethoxy）methyl）-phenol, then further react with isopropylamine, finally react with fumarate to give the target product S-and R- bisoprolol fumarate with a total yield of 60.8% and an ee value is higher than 92%.
出处
《河北科技大学学报》
CAS
北大核心
2010年第4期317-320,共4页
Journal of Hebei University of Science and Technology
基金
河北省科技研究与发展计划项目(09276410D)
