Gyéresi A, Péter M, Fülöp F
Orvosi és Gyógyszerészeti Egyetem, Gyógyszerészeti Kémiai Tanszék, 4300 Târgu-Mures, Gh. Marinescu 38., Románia.
Acta Pharm Hung. 2000 Jul-Dec;70(3-6):138-45.
The applicability of (1R,2R)-1,3-diacetoxy-1-(4-nitrophenyl)-2-propyl isothiocyanate [(R,R)-DANI] as a recently developed chiral derivatizing agent for the enantioseparation of a series of beta-blockers is described. The thiourea diastereomers formed were analysed by reversed-phase high-performance liquid chromatography, mixtures of water and methanol or acetonitrile being used for elution. Conditions of derivatizations (temperature, reagent excess and reaction time) were optimized. The effects of organic modifiers on the retention and separation were investigated; the diastereomers could readily be baseline-separated with methanol-containing mobile phases. The reagent allowed the detection of all four stereoisomers of labetalol, which has two chiral centres.
描述了(1R,2R)-1,3-二乙酰氧基-1-(4-硝基苯基)-2-丙基异硫氰酸酯[(R,R)-DANI]作为一种最近开发的手性衍生化试剂用于一系列β-受体阻滞剂对映体分离的适用性。通过反相高效液相色谱分析形成的硫脲非对映异构体,使用水与甲醇或乙腈的混合物进行洗脱。对衍生化条件(温度、试剂过量和反应时间)进行了优化。研究了有机改性剂对保留和分离的影响;使用含甲醇的流动相可轻松实现非对映异构体的基线分离。该试剂能够检测具有两个手性中心的拉贝洛尔的所有四种立体异构体。