合成2,5-二芳基噻唑衍生物的新方法  

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

作　　者：曾鸿运 张军干 洪伟[1,2] Zeng Hongyun;Zhang Jun'gan;Hong Wei(School of Chemistry and Chemical Engineering,North Minzu University,Yinchuan 750021;Key Laboratory of Chemical Engineering and Technology,State Ethnic Affairs Commission,North Minzu University,Yinchuan 750021)

机构地区：[1]北方民族大学化学与化学工程学院,银川750021 [2]北方民族大学国家民委化工技术基础重点实验室,银川750021

出　　处：《有机化学》2020年第8期2535-2542,共8页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.81660588,81960623);国家民委中青年英才培养计划资助项目。

摘　　要：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.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.

关 键 词：2 5-二芳基噻唑 HECK反应 有机合成 

分 类 号：O626.25[理学—有机化学] TQ460.1[理学—化学]