利用二硝基苯甲酰苯基甘氨酸型手性固定相直接拆分丙卡特罗药物对映体  

Direct Resolution of Procaterol Enantiomers by Using Dinitrobenzoylphenylglycine as a Chiral Stationary Phase

作　　者：郑文丽[1] 宋航[1] 梁彦明[1] 付超[1] 

机构地区：[1]四川大学化工学院制药与生物工程系,四川成都610065

出　　处：《色谱》2003年第3期239-241,共3页Chinese Journal of Chromatography

摘　　要：用手性源(R) 苯基甘氨酸,采用非对称合成方法制备了3,5 二硝基苯甲酰 (R) 苯基甘氨酸手性固定相(DNB PGCPS),利用它直接拆分了丙卡特罗药物的部分对映体,取得了良好的拆分效果。以不同比例的异丙醇 正己烷(体积比分别为20∶80,10∶90,5∶95,2∶98)为流动相,对丙卡特罗进行了拆分,其分离因子α的范围为1 54～1 67。此外,还测试了不同流动相组成对分离效果的影响,考察了液固吸附色谱保留值方程lnk=a+cCb+blnCb中保留因子k和分离因子α与强极性洗脱剂组分b的浓度Cb的关系,对拆分机理进行了讨论。A chiral stationary phase (CSP) 3,5dinitrobenzoylphenylglycine (DNBPG) for liquid chromatographic separation of procaterol enantiomers was prepared by asymmetric synthesis using (R)phenylglycine and 3,5dinitrobenzoyl. DNBPG was covalently bonded to 3aminopropyltriethoxysilane silica. Direct enantiomeric resolution of procaterol hydrochloride was achieved with satisfactory results. The effect of 2propanol contents in the mobile phase on the resolution was determined experimentally. The separation factors obtained were between 154-167 when using different mobile phase compositions of 2propanolhexane (20∶80, 10∶90, 5∶95, 2∶98, v/v) at 26 ℃ and 20 mL/min. The relationship of 2propanol concentration with k and α of procaterol hydrochloride was developed in the fundamental elution equation lnk=a+cCb+blnCb. In addition, by studying the influence of the structural features of DNBPG CSP on enantioselective recognition of procaterol hydrochloride, a hypothetical chiral recognition mechanism was developed. 

关 键 词：二硝基苯甲酰-苯基甘氨酸型手性固定相 手性拆分 丙卡特罗 药物对映体 高效液相色谱法 Β2受体兴奋剂 手性药物 

分 类 号：R914.4[医药卫生—药物化学]