目的探索抗肝炎药(±)-双环醇的不同生物活性,对(±)-双环醇进行拆分。方法采用光学活性生物碱与(±)-双环醇的水解产物(±)-醇酸反应得到一对非对映异构体盐,利用其在溶剂中的不同溶解度分离得到(-)-醇酸光学活性生物碱盐和(+)-醇酸光学活性生物碱盐,分别经酸解离、甲基化,得到(-)-双环醇及(+)-双环醇。结果经熔点、比旋光度、氢核磁共振谱、质谱确定结构,手性柱HPLC测定其光学纯度为100%。结论药理结果显示,(-)-双环醇药理作用为(±)-双环醇的2倍,(+)-双环醇无效。 Objective To explore the different bioactivities of (±) - bicyclol, an anti-hepatitis drug, and to separate (±) - bicyclol. Methods A pair of diastereoisomeric salts were obtained by the reaction of optically active alkaloids with (±) - bicycloalcohol hydrolysates (±) - alkyds and their (-) - alkyd acids were isolated by their different solubilities in solvents The optically active alkaloids salts and (+) - alkyd optically active alkaloids salts are dissociated and methylated respectively by acid to obtain (-) - bicyclol and (+) - bicyclol. Results The structure was confirmed by melting point, specific rotation, proton nuclear magnetic resonance and mass spectrometry. The optical purity was 100% by HPLC. Conclusions Pharmacological results show that pharmacological effects of (-) - bicyclol are 2 times (±) - bicyclol and (+) - bicyclol is not effective.