双氢青蒿素差向异构体转化的研究  

Studies on the Conversion of Epimers of Dihydroartemisinin

作　　者：刘宁 杨腊虎[1] 张正行[2] 俞如英[1] 

机构地区：[1]中国药品生物制品检定所,北京100050 [2]中国药科大学,南京210009

出　　处：《药物分析杂志》2002年第4期303-306,共4页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:对双氢青蒿素β型差向异构体向α型转化过程进行分析。方法:建立高效液相色谱法分离异构体。色谱柱:Kromasil C_(18)柱(250mm×4.6mm,5μm),流动相:乙腈-水(80:20),流速:1.0mL·min^(-1),进样量:20μL,检测波长:216nm。采用LC/MS,LC/NMR对其异构体进行了确证。LC/MS:ESI,扫描:50～1000m/z,干燥气:N_2(10L·min^(-1)),温度:350℃,电压:4000V。LC/NMR:500MHz,溶剂:甲醇。结果:双氢青蒿素在有机溶剂中由β型差向异构体向α型转化并且在一定条件下达到平衡。结论:将双氢青蒿素的α型和β型差向异构体的转化条件及其历程作为双氢青蒿素的手性分离。Objective: Studies on condition of anomeric conversion of β - epimer to α - epimer of dihydroartemisi-nin. Methods: An optioned HPLC condition has developed for separation of the epimers, column; Kromasil C18 (250 mm ×4. 6 mm, 5 μm) ; mobile phase: CH3CN-H2O (80:20), flow rate: 1.0mL·min-1, detector wavelength; 216 nm, injection volume; 20 μL. The epimers were further confirmed by LC/MS, LC/NMR. LC/MS: ESI, SCAN: 50 -1 000 m/z, gas atomspher: N2 ( 10 L · min-1), temperature: 350 ℃, power pressure: 4 000 V. LC/NMR: 500 MHz, solvent: methanol. Results: Dihydroartemisinin has a process of anomeric conversion from the β - epimer to α - epimer in organic solvent and the balance of α, β - anomeric conversion was made. Conclusion: The conversion situation and process of α - and β - epimers were suggested for chiral separation of dihydroartemisinin.

关 键 词：双氢青蒿素 差向异构体 HPLC 手性分离 色谱柱 

分 类 号：R927.1[医药卫生—药学]