3种新型α_1-受体阻断剂的手性流动相HPLC分离与制备  

CHIRAL SEPARATION AND PREPARATION OF THREE NEW ANTAGONISTS OF α_1-ADRENOCEPTORS BY CHIRAL MOBILE PHASE HPLC

作　　者：牛长群[1] 任雷鸣[1] 等 

机构地区：[1]河北医科大学药学院，河北石家庄050017

出　　处：《药学学报》2002年第6期450-453,共4页Acta Pharmaceutica Sinica

基　　金：国家教委留学人员博士后基金 [教外司留 ( 1997) -4 36] .

摘　　要：目的　建立 3种新型α1 受体阻断剂的手性流动相HPLC分离与半制备方法。方法　通过探讨有机相、手性添加剂、流动相的pH、扫尾剂、反相固定相对手性分离的影响 ,选择最佳的手性分离条件。结果　基线分离了 3种新型α1 受体阻断剂对映体 ,并制备了毫克级样品。AIM To establish new methods for the chiral separation and preparation of three new drugs, alfuzosin, terazosin and doxazosin. METHODS By optimizing factors which affect the chiral separation, modifier of solvent, chiral additive, pH of mobile phase, modifier of organic base and stationary phase, the optimum condition for chiral separation were selected. The preparation of enantiomers was carried out on semi preparative reverse phase column (7 8 mm×250 mm C 4 5 μm). Acetonitrile water modified by the addition of carboxymethyl β cyclodextrin (2%～5%, w/v ) was applied as chiral mobile phase. RESULTS The enantiomers of three new drugs were base line separated and milligram scale samples of enantiomer were obtained. CONCLUSION The newly established method can be used in research and development of the enantiomers of three new drugs.

关 键 词：α1-受体阻断剂 手性流动相 HPLC 制备工艺 

分 类 号：TQ460.6[化学工程—制药化工]