自1848年 Pasteur 发现酒石酸光学异构体后,光学活性化合物已引起极大的注意。1987年美国药典药名字典收载的2050种药物中约一半含有一个不对称中心。在生物体内的手性环境中,药物的吸收、分布、代谢和排泄都牵涉到与酶、受体、载体、核酸和多糖的反应,这些生物大分子都具有立体特征结构。也就是说对映体分子应具有不同的生理活性,这种差异不仅表现在药效学而且还影响到药动学模式。美国 FDA 和欧共体等已要求在申报具手性结构的新药时,需要有各对映体的药理、毒理和药动学资料。对映体的理化性质在非手性条件下完全相同,为了分离对映体,手性色谱学应 Optically active compounds have attracted a great deal of attention since the discovery of tartaric acid optical isomers by Pasteur in 1848. About half of the 2050 medicines contained in the 1987 U.S. Pharmacopeia Dictionary contain an asymmetric center. The absorption, distribution, metabolism and excretion of drugs involve the reaction with enzymes, receptors, carriers, nucleic acids and polysaccharides in the chiral environment of the organism. All of these biological macromolecules have the stereospecific structure. In other words, enantiomers should have different physiological activities, this difference not only in the pharmacodynamics but also affect the pharmacokinetic model. The United States FDA and the European Community have demanded that pharmacological, toxicological and pharmacokinetic data for each enantiomer be required when declaring a new drug with a chiral structure. The physical and chemical properties of the enantiomers are exactly the same under achiral conditions. In order to separate the enantiomers, chiral chromatography should