具有抗菌活性Indiacen A的合成研究  

Synthesis of Indiacen A with Antibacterial Activity

作　　者：白梦娇 刘熙 王立花 江世智 雷婷 Bai Mengjiao;Liu Xi;Wang Lihua;Jiang Shizhi;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》2023年第3期64-67,共4页Guangdong Chemical Industry

基　　金：云南省地方本科大学(部分)基础研究联合专项基金项目(No.2019FH001(-087)和202101AO070315)。

摘　　要：设计以4-溴吲哚-3-甲醛为原料,经Vilsmeier-Haack甲酰化反应、Heck-dehydration反应等关键反应步骤,最终合成了具有抗菌活性的Indiacen A。其中三烷基胺盐在Heck-dehydration反应中起关键作用,可促进Indiacen A的中间体脱水。本合成路线具有操作简单、收率高的特点,该方法可用于其他卤代吲哚生物碱的合成,为寻找与开发新的活性药物提供有力支撑。Indiacen A with antibacterial activity is synthesized from 4-bromo-indole-3-formaldehyde by Vilsmeier-Haack formylation reaction,Heck-dehydrogenation reaction and other key reaction steps.Trialkylamine salt plays a key role in Heck-dehydration reaction and can promote the dehydration of the intermediate of Indiacen A.This synthetic route is characterized by simple operation and high yield.This method can be used for the synthesis of other halogenated indole alkaloids,providing strong support for the search and development of new active drugs.

关 键 词：Indiacen A 三烷基胺盐 相转移催化剂 缓冲盐 Heck-dehydration反应 

分 类 号：R914[医药卫生—药物化学]