CAS: 3690-46-8; 5-(Pyridin-3-yl)-1,3,4-Oxadiazole-2-Thiol

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📜烟酸乙酯置于一水合肼,Potassium Hydroxide体系中,用 乙醇 作为反应溶剂,化学反应 13.0H,反应生成 5-(3-吡啶基)-1,3,4-噁二唑-2-硫醇
参考文献:新型5-取代的1,3,4-恶二唑曼尼希碱和双曼尼希碱作为酮醇酸还原异构酶抑制剂的合成及生物活性.
标题:新型5-取代的1,3,4-恶二唑曼尼希碱和双曼尼希碱作为酮醇酸还原异构酶抑制剂的合成及生物活性.
摘要:方便地以高收率方便地合成了一系列新颖的5-取代的1,3,4-恶二唑曼尼希碱和双曼尼希碱.通过ir,(1)h NMR,(13)c NMR和元素分析对它们的结构进行表征.初步的生物测定结果表明,某些化合物对几种试验植物真菌显示出非常好的体外杀真菌活性.其中一些对甘蓝型油菜表现出显着的除草活性,对水稻酮醇-酸还原异构酶(kari)的体外抑制活性极好.在14种新化合物中,8C,8D和8M显示出有效的kari抑制活性,Ki值分别为(0.96+/-0.42),(3.86+/-0.49)和(3.10+/-0.71)μmol/ L,与ipoha相当.这些化合物可能是新型的kari抑制剂,需要进一步研究.
DOI:10.1016/j.Bmcl.2016.08.059

专利信息

专利号:US-4894380-A
优先权日:1987-04-03
标题:2-mercapto-5-pyridyl-1,3,4-oxadiazoles and 2-mercapto-5-pyridyl-1,3,4-thiadiazoles of the formula I
发明人：NYFELER ROBERT; ECKHARDT WOLFGANG; BERIGER ERNST; KRISTIANSEN ODD
权利人:CIBA GEIGY CORP
摘要:The invention relates to 2-mercapto-5-pyridyl-1,3,4-oxadiazoles and 2-mercapto-5-pyridyl-1,3,4-thiadiazoles of the formula I (I) wherein X is oxygen or sulfur, R' is C1-C3alkyl which is substituted by bromine, fluorine, C1-C3alkoxy or cyano; unsubstituted or halogen-substituted C3-C7alkenyl; unsubstituted or halogen-substituted C4-C7alkynyl, R is C1-C3alkyl, unsubstituted C1-C3alkoxy or C1-C3alkoxy which is substituted by halogen or C1-C3alkoxy; unsubstituted or halogen-substituted C3-C7alkenyl; C3-C7alkynyl, C1-C3alkylthio, halogen, cyano, hydroxy, amino or amino which is substituted by one or two C1-C3alkyl groups; or is aminocarbonyl; and n is 0, 1, 2, 3 or 4, to the preparation of the compounds of formula I and to novel intermediates for the synthesis of these compounds. The compounds of formula I have nematicidal properties. The invention further relates to nematicidal compositions which contain at least one compound of formula I as active component, and to methods of using said compounds and of the compositions containing them for controlling nematodes.