构建1,3,5-三嗪环新方法的研究进展  

Progress in New Methods for Construction of 1,3,5-Triazine Ring

作　　者：谭玉敏 刘纤 陈怡诺 黄绍强 曾明 TAN Yumin;LIU Xian;CHEN Yinuo;HUANG Shaoqiang;Zeng Ming(School of Pharmcy and Life Science,Jiujiang University,Jiujang 332005,China)

机构地区：[1]九江学院药学与生命科学学院,江西九江332005

出　　处：《合成化学》2024年第3期288-300,共13页Chinese Journal of Synthetic Chemistry

基　　金：江西省自然科学基金项目(20224BAB206119,20212BAB216070);国家级大学生创新创业训练项目(202211843024,202311843018)。

摘　　要：1,3,5-三嗪类化合物因具有广泛的生物活性如抗肿瘤、抗菌和抗炎等活性,并且目前已有多个以1,3,5-三嗪为母核的小分子抗肿瘤药物被FDA批准或进入临床研究阶段,因此,该类化合物的合成方法受到了广泛的关注。本文总结了近年来构建1,3,5-三嗪环的新方法,并从起始原料不同将这些反应分为3类,即以脒类化合、以胍类化合物和以其他类为原料。这些新方法主要通过[1+2+3](以脒类化合物为原料)或[1+5](以胍类化合物为原料)的成环方式进行三嗪环的构建,具有原子经济性高、绿色环保、操作简单和收率高等优点。本文希望通过对1,3,5-三嗪类化合物合成新方法的总结和归纳,为1,3,5-三嗪环的构建和衍生化提供启发。1,3,5-triazine compounds exhibit various biological activities,such as anti-tumor,antibacterial,anti-inflammatory,etc.At present,several anti-tumor drugs with 1,3,5-triazine as pharmacophore have been approved by FDA or entered the clinical research.Therefore,the synthesis methods of these compounds have attracted considerable attention.This paper summarize new methods for the construction of 1,3,5-triazine ring in recent years.These reactions could be classified into three parts according to the different raw materials,using amidine compounds guanidine compounds as raw materials and other starting materials.These new methods mainly through[1+2+3](with amidine compounds as raw materials)or[1+5](with guanidine compounds as raw materials)coupling annulations for construction of triazine ring and feature highly atom economical,environmentally friendly,operation conveniently and higher conversion.The summary and induction of new methods for the preparation of 1,3,5-triazine will provide inspiration for the construction and derivatization of 1,3,5-triazine rings.

关 键 词：1 3 5-三嗪 合成方法 三嗪环构建 新方法 起始原料 

分 类 号：O626.4[理学—有机化学]