5种甘草次酸衍生物的制备

Preparation of glycyrrhetinic acid derivatives

目的合成制备5种甘草次酸类衍生物,并对其制备工艺进行优化。方法以18β-甘草次酸为原料,分别通过高温碱催化构型转化反应以及硫酸催化酯化反应,合成制备5种甘草次酸类衍生物;利用简单的因素分析法,对5种衍生物的制备工艺进行优化;利用光谱分析法进行结构鉴定。结果通过以上方法分别制得:18β-甘草次酸的光学异构体18α-甘草次酸(产率63%),3-乙酰-18β-甘草次酸(96%),3-乙酰-18α-甘草次酸(90%),18β-甘草次酸甲酯(79%)和18α-甘草次酸甲酯(67%);对各衍生物的理化性质和光谱特征进行详细描述。结论该研究中的制备方法操作工艺简单、原料易得、产率较高,对文献工艺做了一定改进。该研究结果为甘草次酸的深入研究奠定一定基础。

Objective To prepare and characterize 5 glycyrrhetinic acid（GA） derivatives,and to optimize the preparation method.Methods Chemical modification methods were performed for preparing five target compounds with 18β-GA as the starting material;the base catalyzed high temperature and different acetylating methods were used respectively for optical epimerization and esters formation;the routine spectrometric methods were used for chemical structure identification.Results Five target compounds,ie,18α-GA（the optical isomer of 18β-GA,yield 63%）,3-acetyl-18β-GA（yield 96%）,3-acetyl-18α-GA（yield 90%）,18β-GA-30-methyl ester（79%） and 18α-GA-30-methyl ester（67%） were obtained.Their physical-chemical properties and spectrometric characteristics were described.Conclusion These methods possessed certain advantages such as simple operation procedures and high production yields,and have some significance for progressive studies on glycyrrhetinic acid derivatives.