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新型N-(4,6-双取代嘧啶-2-基)-N’-(三氟甲基苯基)胍的合成,结构及生物活性研究
引用本文:何凤琦,刘幸海,王宝雷,李永红,李正名. 新型N-(4,6-双取代嘧啶-2-基)-N’-(三氟甲基苯基)胍的合成,结构及生物活性研究[J]. 中国化学, 2008, 26(8): 1481-1485. DOI: 10.1002/cjoc.200890268
作者姓名:何凤琦  刘幸海  王宝雷  李永红  李正名
作者单位:南开大学元素有机化学研究所,元素有机化学国家重点实验室,农药国家工程中心,,300071, 天津
摘    要:设计,合成了10种新型的胍衍生物,结构经FTIR, MS, 1H NMR 和元素分析确证,并且采用X-射线衍射分析方法确证了具有较好生物活性的化合物11a的结构。并且对这些化合物进行了除草活性测试,结果表明化合物11a,11b,11c在100µg·mL-1 对油菜具有较好的抑制作用,初步的KARI活性结果表明这些化合物对KARI的活性很弱。

关 键 词:合成;三氟甲基苯基胍衍生物;晶体结构;KARI;除草活性
收稿时间:2007-11-06
修稿时间:2008-01-10

Synthesis,Structure and Biological Activities of Some Novel N‐(4,6‐Disubstituted‐pyrimidin‐2‐yl)‐N′‐(trifluoromethylphenyl)‐guanidine Derivatives
Feng‐Qi HE,Xing‐Hai LIU,Bao‐Lei WANG,Yong‐Hong LI,Zheng‐Ming LI. Synthesis,Structure and Biological Activities of Some Novel N‐(4,6‐Disubstituted‐pyrimidin‐2‐yl)‐N′‐(trifluoromethylphenyl)‐guanidine Derivatives[J]. Chinese Journal of Chemistry, 2008, 26(8): 1481-1485. DOI: 10.1002/cjoc.200890268
Authors:Feng‐Qi HE  Xing‐Hai LIU  Bao‐Lei WANG  Yong‐Hong LI  Zheng‐Ming LI
Affiliation:1. State‐Key Laboratory of Elemento‐Organic Chemistry, National Pesticide Engineering Research Center, Institute of Elemento‐Organic Chemistry, Nankai University, Tianjin 300071, China;2. Tel.: 0086‐022‐23503732;3. Fax: 0086‐022‐23505948
Abstract:A novel series of guanidine derivatives were designed, synthesized and confirmed by FTIR, MS, 1H NMR and elemental analysis. The single crystal structure of 11b was determined by X‐ray diffraction. Herbicidal activities of these guanidine derivatives were evaluated through barnyardgrass and rape cup tests, among which compounds 11a , 11b , and 11c against Brassica campestris reached 71.2%, 86.7%, and 86.9% at 100 µg·mL?1 respectively. The preliminary ketol‐acid reductoisomerase test showed that the synthesized compounds had weak activities.
Keywords:synthesis  trifluoromethyl‐phenyl‐guanidine derivative  crystal structure  herbicidal activity  herbicidal activity
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