含苯并杂环芳基硫醚的合成及其抗肿瘤活性研究  

Synthesis and Antitumor Activity of Benzoheterocyclic Aryl Sulfide

作　　者：杨媛[1] 牛丽君 闫泽宇 叶姗姗 张变香[1] Yang Yuan;Niu Lijun;Yan Zeyu;Ye Shanshan;Zhang Bianxiang(School of Chemistry and Chemical Engineering,Shanxi University,Taiyuan,030006)

机构地区：[1]山西大学化学化工学院,太原030006

出　　处：《有机化学》2024年第9期2854-2861,共8页Chinese Journal of Organic Chemistry

基　　金：山西省重点研发计划(No.202202040201009);中央引导地方科技发展基金(No.YDZJSX2021C001)资助项目.

摘　　要：以2-巯基苯并唑类化合物和环状二芳基碘鎓盐为原料,在CuI的催化下成功合成了含苯并杂环的芳硫醚类化合物.采用^(1)H NMR、^(13)C NMR、紫外可见光谱等技术对目标产物进行了表征.探究了反应的最佳条件,生成物最高产率达到了95%.同时,对产物进行了抗肿瘤等生理活性测试,产物表现出良好的抗肿瘤活性.与线性的二芳基碘鎓盐相比,反应中生成的碘苯副产物被有效地固定在生成物中,提高了反应的原子经济性.此外,分子结构中的C—I键为后续反应或者应用提供了明确的反应位点.Aryl thioethers containing benzene heterocycles were synthesized from reaction of 2-mercaptobenzazoles with cyclic diaryl iodonium salts by CuI catalyst.The target products were characterized by ^(1)H NMR,^(13)C NMR and UV-Vis spectroscopies.The optimum reaction conditions were discussed,and the highest yield of the target product reached 95%.The optical properties and physiological activities of the products were also tested and analyzed.At the same time,anti-tumor activity tests were conducted on the products,and some products showed good anti-tumor activity.Compared with linear diaryliodonium salts,the iodobenzene by-product generated in the reaction is immobilized in the product,which improves the atom economy,and the C—I bond in the molecular structure provides a reaction site for subsequent reactions or applications.

关 键 词：2-巯基苯并唑类 环状二芳基碘鎓盐 芳基硫醚 苯并杂环 

分 类 号：TQ460.1[化学工程—制药化工]