手性对氯苄基四氢小檗碱的合成  

Synthesis of Chiral Compounds of 4-Chlorobenzyl Tetrahydroberberine Chloride

作　　者：张灿[1] 林云[1] 华维一[1] 

机构地区：[1]中国药科大学新药研究中心,南京210009

出　　处：《中国药科大学学报》2004年第5期393-396,共4页Journal of China Pharmaceutical University

基　　金：江苏省自然科学基金资助项目 (No .BK2 0 0 2 12 0 )~~

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 86 0 17)的四个光学异构体。结果和结论 :四个光学异构体经IR、1HNMR、13 CNMR、MS。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 raw material,then resoluted with (-)/(+) di-o,o,-p-toluyl-tartaric acid Quaternary ammonium reaction of (-)S and (+)R tetrahydroberberine was conducted by 4-chlorobenzylchloride and four chiral compounds of 4-chlorobenzyl tetrahydroberberine chloride were obtained and separated RESULT AND CONCLUSION:By means of IR, 1 HNMR , 13 CNMR ,MS,elemental analysis and on the basis of the reference,the chemical structures and configurations of four chiral compounds were identified

关 键 词：小檗碱 CPU-86017 季铵化 拆分 手性 

分 类 号：TQ463[化学工程—制药化工]