手性对氯苄基四氢小檗碱的合成

基金项目: 江苏省自然科学基金

Synthesis of Chiral Compounds of 4-Chlorobenzyl Tetrahydroberberine Chloride

摘要: 目的:合成和分离对氯苄基四氢小檗碱的四个异构体,寻找优良的抗心律失常活性新药.方法:以小檗碱为原料进行还原制备四氢小檗碱,并用(-)/( )二对甲苯甲酰酒石酸对其拆分得到(-)S、( )R四氢小檗碱,然后每一单一异构体再进行季铵化,分别得到两个非对映异构体,最后进行柱层析分离制得对氯苄基四氢小檗碱(CPU-86017)的四个光学异构体.结果和结论:四个光学异构体经IR、1HNMR、13CNMR、MS、元素分析及在参考有关文献的基础上确证了其结构和构型.
- 小檗碱 /
- 季铵化 /
- 拆分 /
- 手性
Abstract: AIM:To prepare and separate four chiral compounds of 4-chlorobenzyl tetrahydroberberine chloride (CPU-86017), from which to look for novel potent compounds with antiarrhythmic activity METHOD: Tetrahydroberberine was synthesized by using berberine as r