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齐墩果酸属于齐墩果烷型化合物,是五环三萜类最具有代表性的重要天然活性物质,其各种新型衍生物的设计合成是发展此类药物的重要策略和方法。本文以齐墩果酸为起始物,经过Jones氧化、与甲氧基胺成肟反应以及硼烷-叔丁胺还原等3步反应,合成了3-甲氧基氨基齐墩果烷-12-烯-28-酸。合成路线简单,易于操作,总收率为40%。目标化合物可作为新随机糖苷化反应的苷元。
Oleanolic acid belongs to the oleanane type compound and is the most representative natural active substance of the pentacyclic triterpenoid. The design and synthesis of various novel derivatives are important strategies and methods for the development of such drugs. In this paper, 3-methoxyamino oleanane-12-ene was synthesized from oleanolic acid as starting material through Jones oxidation, oxime reaction with methoxyamine and borane-tert-butylamine reduction. -28-acid. The synthesis route is simple and easy to operate with a total yield of 40%. The target compound serves as aglycone for the new random glycosylation reaction.