文献类型：期刊文献

中文题名：超短效β－肾上腺素受体阻滞剂艾司洛尔的新法合成

英文题名：A New Synthesis of Esmolol,An Ultra-short-acting β-Adrenergic Receptor Blocking Agent

作者：虞鑫红[1];刘丽[1];陈钟瑛[1];刘红[1];仇红花[1];施正娟[1]

机构：[1]华东理工大学药物化工研究所

年份：1995

卷号：5

期号：2

起止页码：150

中文期刊名：中国药物化学杂志

外文期刊名：Chinese Journal of Medicinal Chemistry

收录：CSTPCD;;CSCD:【CSCD_E2011_2012】；

语种：中文

中文关键词：超短效;β-肾上腺素;受体阻滞剂;艾司洛尔;合成

外文关键词：Esmolol; Ultra-short-actingβ-adrenergic blocking agent;Solid-liquid phase transfer catalysis

摘要：本文报道以对羟基苯甲醛为起始原料经缩合、甲酯化、环氧丙基化、异丙胺基化、氢化及成盐等反应合成标题化合物艾司洛尔的新路线。氧上环氧丙基化反应采用液固相转移催化法，副反应少，反应周期短，总收率为５０．３％，艾司洛尔及各中间体的结构均经ＩＲ，１Ｈ－ＮＭＲ和元素分析证实。其中４－（２，３－环氧丙氧基）苯丙烯酸甲酯及３－｛４－［２－羟基－３－（１－甲基乙胺基）丙氧基］苯基｝丙烯酸甲酯未见文献报道。
In this paper,a new route for synthesizing esmolol.an excellent ultra-short-acting β-adrenergic receptor blocking agent is disclosed. para-Hydroxybenzenaldehyde was condensed with maloic acid in toluene in the presence of pyridine,piperidine as well as anilinc,followed by esterification with methanol,O-alkylation with epichlorohydrin by solid-liquid phase transfer catalysis , and amination with isopropylamine , and finally hydrogenated,using 10%Pd-C as a catalyst to prepare the title compound esmolol in 50.3%overall yield.