毒扁豆碱的全合成研究进展

The Research Progress on Total Synthesis of Physostigmine

毒扁豆碱(physostigmine)是已知最早的乙酰胆碱酯酶(AChE)抑制剂,是1864年从非洲西部的毒扁豆种子中分离得到的一种生物碱,具有很好的生物活性,临床主要用于治疗青光眼、阿托品中毒和有机磷中毒,目前还用于治疗阿尔茨海默病(DA)。因此毒扁豆碱及其类似物的合成受到了广泛的关注和研究,目前的研究主要集中在该类化合物三环体系和手性季碳中心的构建。本文综述了近几年来,毒扁豆碱的全合成研究状况。

Physostigmine was the earliest known cholinesterase（AChE） inhibitors,which was a kind of alkaloids firstly isolated from the seeds of the African Calabar bean Physostigma venenosum in 1864.It has well biological activity.In clinic it is mainly used for treating glaucoma,atropine and organophosphate intoxication,now also used to treat alzheimer disease（DA）.Therefore physostigmine and analogues received widespread concerning and research,the present study focused on the construction of three-ring system and quaternary carbon center of this kind of alkaloids.This paper review the prgress on the total synthesis of physostigmine rescent year.