新型2H-噻唑[3,2-b][1,2,4]三嗪-3,7-二酮的超声辅助一锅法合成及乙酰胆碱酯酶抑制活性研究  

One-pot Syntheses of Novel 2H-thiazole [3,2-b] [1,2,4] triazine-3,7-diones Under Ultrasonic Radiation and Their Acetylcholinesterase Inhibitory Activities

作　　者：刘斯婕[1] 赵星[1] 何敬宇[1] 王娟[1] Liu Sijie;Zhao Xing;He Jingyu;Wang Juan(College of Chemical Engineering,Shijiazhuang University,Shijiazhuang,050035)

机构地区：[1]石家庄学院化工学院,石家庄050035

出　　处：《化学通报》2021年第9期981-984,共4页Chemistry

基　　金：河北省自然科学基金项目(H2018106015);河北省杂环类化合物技术创新中心项目(SG2021122)资助。

摘　　要：以取代苯甲醛、溴乙腈和6-苄基-3-硫代-3,4-二氢-1,2,4-三嗪-5(2H)-酮为起始原料,在超声辅助下,一锅法合成了9个新型6-苄基-2-亚苄基-2H-噻唑[3,2-b][1,2,4]三嗪-3,7-二酮类化合物,其结构经^(1)H NMR、^(13)C NMR和MS(ESI)表征,并对其合成机理进行了初步研究。测试了目标化合物4a~4i的体外乙酰胆碱酯酶的抑制活性,其中4a和4d抑制活性最好,有进一步研究的价值。Nine novel 6-benzyl-2-benzylidene-2H-thiazole[3,2-b][1,2,4]triazine-3,7-diones were synthesized by substituted benzaldehyde, bromoacetonitrile and 6-benzyl-3-thio-3,4-dihydro-1,2,4-triazine-5(2H)-one in one pot under the assistance of ultrasound. Their structures were characterized by ^(1)H NMR, ^(13)C NMR and MS(ESI). The synthesis mechanism was preliminarily studied. The acetylcholinesterase inhibitory activities of compounds 4 a~4 i were tested. Among them, compounds 4 a and 4 d have the best inhibitory activities, which are worthy of further studies.

关 键 词：2H-噻唑[3 2-b][1 2 4]三嗪-3 7-二酮 超声辅助 乙酰胆碱酯酶抑制活性 

分 类 号：TQ464.8[化学工程—制药化工]