1，3，4-噻二唑基脲类含氟衍生物的合成及生物活性  

Synthesis and Biological Activity of Fluorinated 1,3,4-Thiadiazolylureas

作　　者：宋新建[1,2] 邵宇 杨平 谭小红[1,2] 余爱农 

机构地区：[1]湖北民族学院生物资源保护与利用湖北省重点实验室,湖北恩施445000 [2]湖北民族学院化学与环境工程学院,湖北恩施445000

出　　处：《精细化工》2012年第3期290-293,共4页Fine Chemicals

基　　金：湖北省自然科学基金(2008CDB016);生物资源保护与利用湖北省重点实验室开放基金(PKLHB1102)~~

摘　　要：以含氟肉桂酸和氨基硫脲为原料、以三氯氧磷为脱水剂,经缩合-环化"一步法"反应制备2-氨基-5-含氟苯乙烯基-1,3,4-噻二唑,再与含氟苯甲酰基叠氮化物反应合成6种1,3,4-噻二唑基脲类含氟衍生物,收率分别为68%、69%、66%、67%、71%和73%。目标化合物的结构用IR、1HNMR、质谱和元素分析进行了表征。初步的生物活性测试表明,目标化合物Ⅲc和Ⅲd在10 mg/L质量浓度下表现出良好的细胞分裂素活性,促进率分别为53.5%和55.1%。Six fluorinated 1,3,4-thiadiazolylureas were synthesized by reaction of fluorine-containing benzoyl azides with 2-amino-5- （ fluorine-containing styryl） -1,3,4-thiadiazoles, which were prepared in one step through the condensation-cyclization of fluorine-containing cinnamic acid thiosemicarbazide with POE13 as dehydrating agent, in the yield of 68%, 69%, 66%, 67%, 71% and and 73% respectively. The structures of the products were confirmed by means of IR,1HNMR, MS and elemental analysis. The preliminary bioassay shows that target compounds III c and m d exhibit good cytokinin activity at the mass concentration of 10 mg/L, and their promoting rates are 53.5% and 55.1% , respectively.

关 键 词：含氟衍生物 4-噻二唑 生物活性 反应合成 脲类 氨基硫脲 1HNMR 细胞分裂素 

分 类 号：TQ453.8[化学工程—农药化工]