紫外光催化合成四氢苯并呋喃衍生物的反应研究  

Synthesis of 2-aminothiophene Derivatives by UV Accelerated Gewald Reaction

作　　者：杨金华 管天冰[1] 夏世豪 周莉佳 李朝政 Yang Jinhua;Guan Tianbing;Xia Shihao;Zhou Lijia;Li Chaozheng(Key Laboratory of Industrial Fermentation Microbiology,Chongqing University of Science and Technology,Chongqing 401331,China)

机构地区：[1]重庆科技学院工业发酵微生物重庆市重点实验室,重庆401331

出　　处：《广东化工》2021年第17期1-2,共2页Guangdong Chemical Industry

基　　金：重庆市研究生科研创新项目资助,编号YKJCX2020515;重庆市教育委员会-科学技术研究项目NO.KJQN201901501;工业发酵微生物重庆市重点实验室开放基金,NO.GYFJWSW-06。

摘　　要：四氢苯并呋喃衍生物是重要的医药中间体,目前其合成方法研究具有局限性。为了获得较好的合成方法,本文将对四氢苯并呋喃衍生物的合成方法进行研究。以环己酮衍生物与氰乙酸乙酯、单质硫为模型反应,经紫外催化,通过考察反应用碱、反应时间和反应温度,确定了最佳条件,并对反应条件进行普适性研究。研究发现该反应条件更加温和,副反应较少,产率较高;小位阻的环己酮衍生物对该条件具有更好的适应性,若反应底物的位阻增大会降低收率。本文报道的四氢苯并呋喃衍生物的合成方法将在医药中间体的合成中具有较好的应用前景。Tetrahydrobenzofuran derivatives are important pharmaceutical intermediates,but their synthesis methods are limited at present.In order to obtain a better synthesis method,the synthesis method of tetrahydrobenzofuran derivatives will be studied in this paper.Using ethyl cyanoacetate and elemental sulfur as models,the best reaction conditions were determined by UV catalysis,and the reaction temperature,reaction time and reaction temperature were investigated.The general applicability of the reaction conditions was studied.It was found that the reaction conditions were milder,side reactions were less,and the yield was higher.Cyclohexanone derivatives with small steric hindrance have better adaptability to this condition,and the yield will be reduced if the steric hindrance of the substrate increases.The synthesis method of tetrahydrobenzofuran derivatives reported in this paper will have a good application prospect in the synthesis of pharmaceutical intermediates.

关 键 词：2-氨基噻吩衍生物 Gewald反应 紫外 有机合成 碱催化 

分 类 号：TQ[化学工程]