消旋-循环拆分法在手性药物合成中的应用  

Application of Recycle Process of Resolution-racemization in Synthesis of Chiral Drugs

作　　者：吕训磊 林快乐[1] 周伟澄[1] LYU Xunlei;LIN Kuaile;ZHOU Weicheng(Shanghai Key Lab.of Anti-infectives,State Key Lab.of New Drug and Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 201203)

机构地区：[1]中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海市抗感染药物研究重点实验室,上海201203

出　　处：《中国医药工业杂志》2023年第2期175-181,共7页Chinese Journal of Pharmaceuticals

摘　　要：拆分是制备手性药物的经典方法。由于拆分剂价格低廉易得、方法成熟、操作简便、易于大规模生产等优势,拆分在制药工业生产中仍然具有一定的地位,但其主要缺点是有另一半不需要的对映异构体产生,造成很大浪费。在消旋化后进行循环拆分,是弥补这个缺点的直接、有效途径。该文主要按不同的消旋化机制[碳负(或正)离子机制和消除还原机制],综述了消旋-循环拆分法在手性药物合成中的应用。The classic resolution of racemates is one of the choices for production of chiral compounds in large scale.Due to the advantages of inexpensive and readily available of resolution agents,mature methods,simple operation,and ease of large-scale production,resolution still plays a role in the pharmaceutical industry.However,its main disadvantage is that half of the products are unwanted enantiomers,resulting in significant waste.Recycle process of resolution-racemization is a direct and effective way to remedy this disadvantage.In this paper,the applications of recycle process of resolution-racemization in synthesis of chiral drugs are reviewed based on the different mechanisms of racemization(carbanion/carbocation mechanism and mechanism of elimination-reduction).

关 键 词：消旋化 循环拆分 碳负(或正)离子机制 消除还原机制 

分 类 号：O658[理学—分析化学] TQ463[理学—化学]