论文部分内容阅读
在大多情况下,对映体(Enantiomers)的差别为:(1)生物活性——这是由于与受体(实质上是蛋白质,也具有手性中心)相互作用的强度不同;(2)转运机制;(3)可能的代谢途径。据统计,常用的200种处方用药中,有114种药物具有至少一个不对称中心,因此,开始试验一个药物时,就有必要将对映体拆分,以确定其效价、毒性和/或不良反应。对映体的拆分有两种基本方法:(1)采用能够区分对映体分子的色谱系统;(2)利用对映体分子中的反应基团与某一光学纯试剂反应产生非对映光学异构体混合物。由于非对映体(Diastereoisomers)之间有较大的物理性质差异,使有可能用非手性色谱系统将其分离,其程
In most cases, the differences between enantiomers are: (1) biological activity - due to differences in the strength of interaction with receptors (essentially proteins, but also with chiral centers); (2) transport Mechanism; (3) possible metabolic pathways. According to statistics, of the 200 commonly prescribed medications, 114 have at least one asymmetric center, so when starting to test a drug, it is necessary to split the enantiomer to determine its potency, toxicity and / or Adverse reactions. There are two basic methods for the resolution of enantiomers: (1) the use of a chromatographic system that separates enantiomeric molecules; (2) the use of enantiomeric reactive groups with an optically pure reagent to produce diastereomers Optical isomer mixture. Due to the large physical differences between diastereoisomers, it is possible to separate them with achiral chromatography systems,