吲哚生物碱Luteoride B的半合成反应研究  

Study on Semi Synthetic Reaction of Indole Alkaloid Luteoride B

作　　者：宋进婕 鹿贵东 杨斌全 雷婷 Song Jinjie;Lu Guidong;Yang Binquan;Lei Ting(College of Pharmacy,Dali University,Dali 671000;Yunnan Key Laboratory of Screening and Research on Anti-pathogenic Plant Resources from West Yunnan(Cultivation),Dali University,Dali 671000,China)

机构地区：[1]大理大学药学院,云南大理671000 [2]云南省滇西抗病原植物资源筛选研究重点实验室(培育),云南大理671000

出　　处：《广东化工》2022年第12期33-36,共4页Guangdong Chemical Industry

基　　金：云南省地方本科高校(部分)基础研究联合专项资金项目(No.2019FH001(-087));云南省滇西抗病原植物资源筛选研究重点实验室(培育)(APR202107)。

摘　　要：LuteorideB是一种具有潜在生物活性的吲哚生物碱,因其含有在天然产物中少见的异戊二烯基团和(E)-肟基结构而受到化学家和药物化学工作者的关注。氨解反应是利用胺化剂将有机化合物上已有的取代基原位反应置换成氨基,在全合成中受到广泛的应用。本文讨论了在半合成Luteoride B的过程中所用到的氨解反应,对常见的几种胺化剂进行讨论,并创新性的添加阻聚剂来减少反应物聚合来提高反应产率。本文报道的氨解反应对该反应在有机合成领域的进一步应用有非常大的价值。Luteoride B is an indole alkaloid with potential biological activity because it contains isoprene groups and(E)-oxime group structure has attracted the attention of chemists and pharmaceutical chemists.Aminolysis is the in-situ reaction of substituents on organic compounds to replace amino groups by aminating agents,which is widely used in total synthesis.In this paper,the ammonolysis of Luteoride B is discussed,several common aminating agents are discussed,and innovative inhibitors are added to reduce the polymerization of reactants to increase the yield.The aminolysis reaction reported in this paper is of great value for its further application in organic synthesis.

关 键 词：吲哚生物碱 Luteoride B 氨解反应 天然产物 半合成 

分 类 号：R914.5[医药卫生—药物化学]