20(S)-原人参二醇氨基酸衍生物的合成

The Synthesis of 20(S)-Protopanaxadiol Amino Acid Derivatives

目的对20(S)-原人参二醇进行结构修饰,合成其氨基酸衍生物,从而提高药物的水溶性。方法以二环己基碳化二亚胺为催化剂、吡啶为溶剂进行反应,合成20(S)-原人参二醇的氨基酸衍生物。结果得到20(S)-原人参二醇的氨基酸衍生物14个,其结构通过1H-NMR、13C-NMR图谱进行确证,同时总结了20(S)-原人参二醇的氨基酸衍生物的合成规律。结论本方法合成工艺简单易行,操作简便,适合工业化生产,所得产物的水溶性较合成前有所提高,有利于提高生物利用度。

OBJECTIVE To improve the water solubility of 20（S）-protopanaxadiol（PPD） by synthesized with a few kinds of amino acids.METHODS In the synthetic reaction,dicyclohexyl carbodiimide was used as the accelerant and pyridine was the solvent.RESULTS Fourteen derivatives had been synthesized and their chemical structures were identified by 1H-NMR and 13C-NMR.Then the rule of this reaction was summarized.CONCLUSION The method is simple,effective,and reproducible,which is benefit to improve the bioavailability of the drug,and the derivatives have better water solubility than PPD.