摘要
目的探讨手性拆分法中化学拆分法的影响因素。方法通过对手性药物的经典拆分方法-化学拆分法相关的文献进行分析整理,探讨利用化学拆分法进行拆分过程中的影响因素。结果手性拆分试剂的种类直接决定了拆分结果,可以根据底物的结构特征选择合适的手性拆分试剂。拆分溶剂的种类也对拆分具有直接的影响,不同的拆分溶剂可能得到构型相反的异构体。拆分试剂与样品的摩尔比可以影响中间体盐的形成及拆分样品的纯度。结论总结归纳的化学拆分法的影响因素,为今后利用化学拆分法开发具有光学活性的药物,设计高效合理的拆分路线提供了有利的参考和依据。
Objective To discuss the influencing factors of chemical resolution methods for chiral drugs.Methods According to the literature on chemical resolution methods for separation of chiral drugs,the influencing factors of chemical resolution methods were analyzed and discussed.Results The manipulated parameters for chiral separation mainly include:resolution agent,resolution solvent,molar ratio of resolving agent to racemic compound.The resolution is directly determined by the resolution agent,while different resolution solvent may result in the opposite isomers.The molar ratio of resolving agent to racemic compound could affect the formation of the intermediate salt and the purity of the sample.Conclusion The paper provides basis for rational design of chemical resolution method for the separation of chiral drugs.
作者
邓艳芳
吴桐
李泽文
李思思
胡雨函
李畅
裴月湖
DENG Yanfang;WU Tong;LI Zewen;LI Sisi;HU Yuhan;LI Chang;PEI Yuehu(College of Pharmacy,Harbin Medical University,Harbin 150081,China)
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2019年第11期1056-1060,共5页
Journal of Shenyang Pharmaceutical University
基金
黑龙江省博士后科学基金资助项目(LBH-Z17178)
黑龙江省省属高等学校基本科研业务费基础研究项目(2017JCZX55)
黑龙江省大学生创新创业训练计划项目(201710226074).
关键词
手性药物
化学拆分
拆分试剂
拆分溶剂
chiral drugs
chemical resolution
resolution agent
resolution solvent
