应用化学

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水相中苯并噻唑类衍生物的微波辐射合成

柯方1*,吴雯2,李鹏1,林晨1   

  1. (1.福建医科大学药学院 福州 350004;2.厦门市妇幼保健院 厦门 361003)
  • 收稿日期:2013-07-17 修回日期:2013-09-01 出版日期:2014-06-10 发布日期:2014-06-10
  • 通讯作者: 柯方,讲师; Tel/Fax:0591-22862016; E-mail:kefang612@163.com; 研究方向:药物化学,催化化学
  • 作者简介: a
  • 基金资助:
    国家自然基金资助项目(81202560);福建省自然基金资助项目(2012J05150)

Microwave-assisted Synthesis of Benzothiazole Derivatives in Aqueous Solution

KE Fang1*, WU Wen2, LI Peng1, LIN Chen1   

  1. (1.Department of Pharmacy,Fujian Medical University,Fuzhou 350004,China;
    2.Xiamen Maternity and Child care Hospital,Xiamen 361003,China)
  • Received:2013-07-17 Revised:2013-09-01 Published:2014-06-10 Online:2014-06-10
  • About author:

    Supported by Natural Science Foundation of China(81202560); Fujian Provincial Foundation (2012J05150). Corresponding gauthor: Tel/Fax:0591-22862016; E-mail:kefang612@163.com; Research interests: pharmaceutical chemistry, catalytic chemistry

摘要: 在水相中建立了一种简单实用,廉价的2-碘芳胺与芳醛和硫氰酸钾反应生成苯并噻唑衍生物的微波辅助铜催化体系。该体系只需以碘化亚铜和1,10-菲罗啉为催化剂,以碳酸铯为碱的100 ℃水中反应30 min,就能得到大量苯并噻唑衍生物,最高产率达94%。

关键词: 微波辅助合成, 碘芳胺, 芳醛, 苯并噻唑

Abstract: A novel protocol, efficient, inexpensive for the microwave-assisted copper-catalyzed synthesis of benzothiazoles derivatives through the reaction of 2-iodoanilines with aldehydes and KSCN in aqueous solution was investigated. The reactions was catalyzed by a combination of CuI and 1,10-phenanthroline with Cs2CO3 as a base and in neat water at 100 ℃ for 30 min. A variety of benzothiazoles can be synthesized in an excellent yield up to 94%.

Key words: microwave-assisted synthesis, iodoaniline, aldehyde, benzothiazoles

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