7-溴异喹啉-1-醇的合成
详细信息    查看全文 | 推荐本文 |
  • 英文篇名:Synthesis of 7-Bromoisoquinolin-1-ol
  • 作者:徐淑周 ; 李福荣 ; 王琛 ; 李忠 ; 谢洪磊
  • 英文作者:XU Shu-zhou;LI Fu-rong;WANG Chen;LI Zhong;XIE Hong-lei;Yantai Institute of Materia Medica,Yantai Key Laboratory of Nanomedicine & Advanced Preparations;Taishan Medical College of Pharmacy;
  • 关键词:异喹啉 ; 苯甲醛 ; 合成
  • 英文关键词:isoquinoline;;benzaldehyde;;synthesis
  • 中文刊名:HNHG
  • 英文刊名:Fine Chemical Intermediates
  • 机构:烟台药物研究所烟台市纳米药物与高端制剂重点实验室;泰山医学院药学院;
  • 出版日期:2019-02-28
  • 出版单位:精细化工中间体
  • 年:2019
  • 期:v.49;No.238
  • 基金:烟台市科技局项目资助(2019MSGY128)
  • 语种:中文;
  • 页:HNHG201901007
  • 页数:3
  • CN:01
  • ISSN:43-1354/TQ
  • 分类号:30-32
摘要
以3-溴苯甲醛和氨基乙醛缩二甲醇起始原料,经Pictet-Gams反应、过氧化反应以及自由基反应得到7-溴异喹啉-1-醇,总收率35%。由核磁共振和质谱对产物进行结构表征。本方法具有反应条件温和、收率高、易于纯化的特点,为7-溴异喹啉-1-醇的合成提供了新途径。
        The titled compound was synthesized using 3-bromobenzaldehyde and 2,2-dimeth-oxyethan-1-amine as the starting materials via Pictet-Gams, peroxidation and radical reaction. The total yield was 35%.The products were characterized using1 H NMR and MS. This synthetic route had the advantages including mild conditions, high yield and easy purification.
引文
[1]CzakoB,Kurti L,Mammoto A.Discovery of potent and practical antiangiogenic agents inspired by cortistatin A[J].Am Chem Soc,2009,131(25):9 014-9 019.
    [2]McCall J M,Kelly R C,Romero D L.Heterocyclic compounds for the inhibition of PSK:US,20120277224[P].2012-02-01.
    [3]Nakamura Y,Hayashi N,Higashijima T.Trisubstituted amine compounds as inhibitors of cholesteryl ester transfer transfer protein CETP:WO,2007088996[P].2007-08-09.
    [4]Sin N,Venables B L,Sun L Q.Heptitis C Virusinhibitors:US,20080119461[P].2008-03-22.
    [5]Langhals H,Naumann C,Ruppertshain K.Bipyridyls and their use as INKS:US,005266700[P].1993-11-30.
    [6]Scola P M,Sun L Q,Wang A X.The discovery of asunaprevir(BMS-650032),An orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.[J].Med Chem,2014,57(5):1 730-1 752.
    [7]Pedras M S C,Abdoli A,Sarma-mamillapalle V K.Inhibitors of the detoxifying enzyme of the phytoalexin brassinin based on quinoline and isoquinoline scaffolds[J].Molecules,2017,22(8):1 345-1 360.
    [8]Koltunov K Y,Surya G K,Rasul G.Superacidic activation of 1-and 3-isoquinolinols and their electrophilic reactions[J].Org Chem,2002,67(25):8 943-8 951.
    [9]Dios D,Paredes G,Garmendia L.Pyrazole-isoquinoline urea derivatives as P38 kinase inhibitors:WO,2007053346[P].2006-10-23.
    [10]Shi J,Manolikakes G,Yeh C.Scalable synthesis of cortistatin a and related structures[J].Am Chem Soc,2011,33(20):8 014-8 027.
    [11]陈建新,王瑾瑾,刘腾蛟,等.6,7-二甲氧基异喹啉-1-甲酸乙酯的高效合成[J].精细化工中间体,2014,44(3):23-25.

© 2004-2018 中国地质图书馆版权所有 京ICP备05064691号 京公网安备11010802017129号

地址:北京市海淀区学院路29号 邮编:100083

电话:办公室:(+86 10)66554848;文献借阅、咨询服务、科技查新:66554700