基于槟榔生物碱骨架设计合成新型δ-内酰胺衍生物  

Design and preparation of areca alkaloid derivativs

作　　者：周吴靓云 陈晨 王萌[1] 杨倩倩 黄维[1] ZHOU War-jingyun;CHEN Chen;WANG Meng;YANG Qian-gian;HUANG Wei(School of Pharmacy,Chengdu University of Trodlitional Chinese Medicine,Chengdu 611137,Sichuan)

机构地区：[1]成都中医药大学药学院,四川成都611137

出　　处：《中药与临床》2023年第3期10-13,共4页Pharmacy and Clinics of Chinese Materia Medica

基　　金：国家自然科学基金(22001024)。

摘　　要：目的:设计并制备槟榔生物碱衍生物。方法:将简单易得的氮杂二烯与恶唑酮作为原料,以磷酸作有机催化剂,发生[4+2]环加成反应,生成苯甲酰胺类δ-内酰胺化合物。结果:合成得到了11个结构新颖的槟榔生物碱衍生物,目标化合物结构经^(1)H-NMR、^(13)C-NMR和HRMS确定。结论:用磷酸作有机催化剂,可制备得到一系列结构新颖且具有苯甲酰胺及磺胺结构的槟榔生物碱衍生物,为后续抗菌消炎活性结构研究提供思路。Objective:To design and prepare areca alkaloid derivatives.Method:[4+2]cycloaddition reaction was carried out with easily obtained azadiene and oxazolone as raw materials and phosphoric acid as an organic catalyst to produce benzamideδ-lactam compounds.Result:1l novel alkaloid derivatives of areca nut were synthesized.The structure of the target compound was determined by^(1)H-NMR,^(13)C-NMR,and HRMS.Conclusion:Using phosphoric acid as the organic catalyst,a series of areca alkaloid derivatives with novel structures and benzamide and sulfonamide structure can be prepared,which provides ideas for the subsequent study of antibacterial and anti-inflammatory activity structure.

关 键 词：槟榔生物碱 结构修饰 δ-内酰胺衍生物 

分 类 号：R282.1[医药卫生—中药学]