新型含2-取代-1,3-噻唑烷环的噻唑酰胺类化合物的合成与生物活性研究  

Synthesis and Bioactivities of Novel Thiazole Amide Derivatives Containing a 2-Substituted-1,3-thiazolidine Ring

作　　者：戴红[1,2] 刘建兵[1] 苗文科[1] 吴珊珊[1] 张欣[1] 王婷婷[1] 方建新[1] 

机构地区：[1]南开大学元素有机化学国家重点实验室,天津300071 [2]南通大学化学化工学院,南通226019

出　　处：《有机化学》2011年第11期1943-1948,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.20772068);南通市科技计划(Nos.K2010016;AS2010005);南通大学自然科学基金(Nos.09Z010;09C001)资助项目

摘　　要：为了寻找新的含噻唑杂环的先导化合物,利用4-[(2-氰基亚胺基-1,3-噻唑烷-3-基)甲基]-2-氨基噻唑与取代苯甲酰氯(或乙酰氯)在吡啶存在下发生缩合反应,合成了19个新型含2-取代-1,3-噻唑烷环的噻唑酰胺类化合物4.经1HNMR和元素分析对目标化合物的结构进行了表征,经MS进一步证实了化合物4s的结构,并通过X射线单晶衍射分析测定了化合物4a的晶体结构.对所合成的目标化合物进行了生物活性测试,部分化合物表现出一定的杀菌和植物生长调节活性.In order to find novel thiazole-heterocycle lead compounds,nineteen new thiazole amides 4 containing 2-substituted-1,3-thiazolidine were synthesized from a condensation reaction of 2-cyanoimino-3-（2-aminothiazol-4-ylmethyl）thiazolidine with substituted benzoyl chlorides（or acetyl chloride）.The struc-tures of these compounds were confirmed by 1H NMR spectra and elemental analysis.The structure of 4s was further characterized by MS technique.The structure of 4a was also determined by X-ray diffraction analysis.Biological activities of the title compounds was tested,and some compounds displayed certain fun-gicidal and plant growth regulatory activities.

关 键 词：2-取代-1 3-噻唑烷 噻唑 酰胺 合成 生物活性 

分 类 号：TQ450.2[化学工程—农药化工]