有机化学 ›› 2020, Vol. 40 ›› Issue (8): 2535-2542.DOI: 10.6023/cjoc202004020 上一篇    下一篇

研究简报

合成2,5-二芳基噻唑衍生物的新方法

曾鸿运a, 张军干a, 洪伟a,b   

  1. a 北方民族大学化学与化学工程学院 银川 750021;
    b 北方民族大学国家民委化工技术基础重点实验室 银川 750021
  • 收稿日期:2020-04-13 修回日期:2020-05-22 发布日期:2020-06-01
  • 通讯作者: 洪伟 E-mail:hongwei@nmu.edu.cn
  • 基金资助:
    国家自然科学基金(Nos.81660588,81960623)和国家民委中青年英才培养计划资助项目.

New Method for the Synthesis of 2,5-Diaryl Substituted Thiazoles

Zeng Hongyuna, Zhang Jun'gana, Hong Weia,b   

  1. a School of Chemistry and Chemical Engineering, North Minzu University, Yinchuan 750021;
    b Key Laboratory of Chemical Engineering and Technology, State Ethnic Affairs Commission, North Minzu University, Yinchuan 750021
  • Received:2020-04-13 Revised:2020-05-22 Published:2020-06-01
  • Supported by:
    Project supported by the National Natural Science Foundation of China (Nos. 81660588, 81960623) and the National Ethnic Affairs Commission Young Talent Training Program.

噻唑环作为一类重要的五元芳香杂环,其衍生物具有多种生物活性,被广泛应用在医药方面.以价廉易得的不同取代苯甲酸为原料,经酰化反应、硫代反应、环合反应和Heck反应合成了2,5-二芳基噻唑衍生物.重点在于优化Heck反应的条件,进行可能反应机理的探讨.该方法具有反应条件温和、操作简单及底物的普适性良好等优点,为2,5-二芳基取代噻唑类化合物的合成提供了新的方向.

关键词: 2,5-二芳基噻唑, Heck反应, 有机合成

Thiazole ring is an important five-membered aromatic heterocyclic ring, and its derivatives have various biological activities and are widely used in medicine. The synthesis of 2,5-diarylthiazole derivatives by acylation, thiolation, cyclization and Heck reaction using inexpensive and readily available substituted benzoic acid as raw materials was developed. The key point was to optimize the Heck reaction conditions and explore the possible reaction mechanism. The method has mild reaction conditions, simple operation, and good substrate universality, which provides a new direction for the synthesis of 2,5-diaryl substituted thiazoles.

Key words: 2,5-diarylthiazole, Heck reaction, organic synthesis