7-氮杂吲哚及其衍生物5-溴-7-氮杂吲哚的合成  

Synthesis of 7-Azaindole and 5-Bromo-7-azaindole

作　　者：郑从燊[1] 陈夏琴[1] 余辉[1] 黄捷[1] 杨帆 汤杰 ZHENG Cong-shen;CHEN Xia-qin;YU Hui;HUANG Jie;YANG Fan;TANG Jie(1.Fujian Institute of Microbiology,Fuzhou 350007,China;School of Chemistry and Molecular Engineering,East China Normal University,Shanghai 200241,China)

机构地区：[1]福建省微生物研究所,福建福州350007 [2]华东师范大学化学与分子工程学院,上海200241

出　　处：《化学试剂》2019年第6期633-636,共4页Chemical Reagents

基　　金：福建省属公益类科研院所基本科研专项资助项目(2017R1009-10)

摘　　要：7-氮杂吲哚是一种重要的杂环化合物,是合成维罗非尼、ABT-199等抗肿瘤药物的重要中间体,具有较高的生物医药价值。优化了合成7-氮杂吲哚的方法,以廉价易得的2-氨基-3-甲基吡啶为起始原料,经过两步反应,以48%的总收率得到7-氮杂吲哚。并在此合成方法的基础上进一步合成了5-溴-7-氮杂吲哚,经过三步反应,总收率达到43%。该合成方法具有原料易得、操作简便、路线简短、收率较高等优点。产物的结构经过核磁共振和高分辨质谱得到确认。7-Azaindole compounds are important heterocyclic compounds,used for the synthesis of vemurafenib and ABT-199.It has high value of biological medicine.New methods for the synthesis of 7-azaindole is reported herein.7-Azaindole is synthesized from 2-amino-3-methylpyridine via a two-step synthetic route in an overall yield of 48%.5-Bromo-7-azaindole is synthesized from 2-amino-3-methylpyridine via a three-step synthetic route in an overall yield of 43%.The product is characterized by NMR and HRMS.The advantages of synthsis are simplified operational procedure,short reaction steps,good yields and the raw materials easy to get.

关 键 词：7-氮杂吲哚 5-溴-7-氮杂吲哚 杂环 合成 

分 类 号：O626.32[理学—有机化学]