摘要
目的 建立手性包甲素类似物绝对构型的简便方法。方法 以外消旋6β-羟基莨菪烷-3-酮为原料,通过拆分、酰化和还原制备手性包甲素类似物。结果 合成了手性包甲素类似物,通过物理常数、光谱数据鉴定其结构并与已知构型的化合物Is进行化学关联确定其绝对构型。结论 本文建立的方法可用于确定某些活性手性包甲素类似物的绝对构型,从而有助于此类化合物构效关系的进一步研究。
Objective To develop a simple and convenient method for determination of abso- lute configurations of certain chiral analogs of Baogongteng - A(BGT-A). Methods To prepare chiral analogs of BGT-A by resolution, acetylation and reduction, using racemic 6β-hydroxy-3-tropinone as starting material. Results We synthesized chiral analogs of BGT-A and confirmed their structures by physical constants and spectral data and absolute configurations by chemical correlation with the com- pound Is, the configuration of which had been known and established. Conclusion Our method could be used to confirm the absolute configuration of some chiral analogs of BGT-A with biological activity, and is useful for further investigation into structure-activity relationship.
出处
《上海第二医科大学学报》
CSCD
2001年第3期199-201,205,共4页
Acta Universitatis Medicinalis Secondae Shanghai
基金
上海市教委重点学科基金资助项目(S970204)
关键词
包甲素类似物
绝对构型
手性化合物
analogs of Baogongteng A
absolute configuration
chiral