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.
出处
《中国药物化学杂志》
CAS
CSCD
1995年第2期150-152,共3页
Chinese Journal of Medicinal Chemistry
关键词
超短效
β-肾上腺素
受体阻滞剂
艾司洛尔
合成
Esmolol
Ultra-short-actingβ-adrenergic blocking agent
Solid-liquid phase transfer catalysis
