2-(4,5-二氢异恶唑-5-基)-1,3,4-恶二唑的合成与生物活性
Synthesis and biological activity of 2-(4,5-dihydroisoxazol-5-yl)-1,3,4-oxadiazoles.
作者信息
Milinkevich Kristin A, Yoo Choong L, Sparks Thomas C, Lorsbach Beth A, Kurth Mark J
机构信息
Department of Chemistry, One Shields Ave., University of California, Davis, CA 95616, USA.
出版信息
Bioorg Med Chem Lett. 2009 Oct 1;19(19):5796-8. doi: 10.1016/j.bmcl.2009.07.139. Epub 2009 Aug 6.
Acid hydrazides were coupled with acrylic acid derivatives and cyclodehydration gave 1,3,4-oxadiazoles. Lastly, in-situ nitrile oxide formation from aryl oximes treated with sodium hypochlorite, and subsequent 1,3-dipolar cycloaddition to the exomethylene moiety delivered 2-(4,5-dihydroisoxazol-5-yl)-1,3,4-oxadiazoles. This library was evaluated in a high-throughput screen at Dow AgroSciences. Several compounds were active against fungal pathogens and pest insects.
酰肼与丙烯酸衍生物偶联，经环脱水反应生成1,3,4-恶二唑。最后，用次氯酸钠处理芳基肟原位生成腈氧化物，随后与亚甲基部分进行1,3-偶极环加成反应，得到2-(4,5-二氢异恶唑-5-基)-1,3,4-恶二唑。该化合物库在陶氏益农公司进行了高通量筛选。几种化合物对真菌病原体和害虫具有活性。
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