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前期,我们以20(S)-PPT 为原料,设计经乙酰化、m-CPBA 氧化和皂化反应,得到近乎等物质量的ocotillol(3)及其C24 差向异构体(4)。经X-ray 单晶衍射证实,3 的C24 为R 构型,4 的C24 为S 构型[1]。
Ocotillol 及其C24差向异构体的合成与形成机理探讨
【摘 要】
：
前期,我们以20(S)-PPT 为原料,设计经乙酰化、m-CPBA 氧化和皂化反应,得到近乎等物质量的ocotillol(3)及其C24 差向异构体(4)。经X-ray 单晶衍射证实,3 的C24 为R 构型,4 的C24 为S 构型[1]。
【机 构】
：
烟台大学药学院,烟台,264005
【出 处】
：
2015年全国药物化学学术会议暨第五届中英药物化学学术会议
【发表日期】
：
2015年3期
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研究表明，源于原人参二醇的C24 差向异构ocotillol 型人参皂苷的心肌保护作用和ADME 存在显著立体差异[1]。有关其半合成的研究已有报道，但其形成机理的研究报道较少。
以20(S)-原人参二醇和为20(S)-原人参三醇原料,经乙酰化、m-CPBA 氧化和氢氧化钠皂化三步反应,合成得到两对ocotillol 型C24 差向异构体1、2 以及3、4,用1H NMR、13CNMR、HMBC、NOESY 及MS 确证其结构,并通过X-ray 单晶衍射确证差向异构体的立体结构[1]。