普萘洛尔乙烯酯前药的高效液相色谱对映体分离  

Chiral Separation of Propranolol Vinyl Ester Prodrug by High Performance Liquid Chromatography

作　　者：权静[1] 陈志春[1] 吴起[1] 王娜[1] 林贤福[1] 

机构地区：[1]浙江大学化学系,杭州310027

出　　处：《分析化学》2006年第U09期78-82,共5页Chinese Journal of Analytical Chemistry

基　　金：国家自然基金资助项目(No.20474056)

摘　　要：利用OD-H手性柱对普萘洛尔及其3种氨基取代和3种羟基取代的普萘洛尔二酸乙烯酯(N-酰基、O-酰基普萘洛尔丁二酸乙烯酯、N-酰基、O-酰基普萘洛尔己二酸乙烯酯、N-酰基、O-酰基普萘洛尔癸二酸乙烯酯)进行了对映体分离的研究。考察了流动相正己烷中不同醇类添加剂、二乙胺、不同的流速以及不同底物结构对分离的影响,并初步探讨了手性分离机理。结果表明,普萘洛尔、3种不同链长的氨基取代普萘洛尔二酸乙烯酯、以及羟基取代的普萘洛尔己二酸乙烯酯在实验的条件下能够达到基线分离。Enantioseparations of propranolol, N-acyl and O-acyl propranololvinyl ester derivatives, including N-acyl and O-acyl propranolol vinylsuccinate, N-acyl and O-acyl propranolol vinyladipate, N-acyl and O-acyl propranololvinylsebacate, which could be useful for the preparation of macromolecular propranolol prodrugs, were carried out on chiral OD-H column. The influences of the concentration and kind of alcohols, concentration of diethylamine, flow rate and different structure on enantioseparation of propranolol and its derivatives were studied. Then chiral separation mechanism of these drugs was also discussed. The results showed that propranolol, N-acyl propranolol vinyl ester derivatives and O-acylpropranolol vinyladipate were separated successfully, while O-acyl propranolol vinylsuccinate and O-acyl propranolol vinylsebacate didn＇t get baselinechiral separation.

关 键 词：高效液相色谱 对映体分离 普萘洛尔乙烯酯 

分 类 号：R917[医药卫生—药物分析学]