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2-取代氨基-5-吡唑基-1,3,4-噁二唑的合成及生物活性
引用本文:袁德凯,李正名,赵卫光,陈寒松. 2-取代氨基-5-吡唑基-1,3,4-噁二唑的合成及生物活性[J]. 应用化学, 2003, 20(7): 624-628
作者姓名:袁德凯  李正名  赵卫光  陈寒松
作者单位:南开大学
基金项目:“八六三”计划 ( #2 0 0 1AA2 3 5 0 11),天津大学 /南开大学联合研究项目资助课题
摘    要:取代氨基吡唑基噁二唑;2-取代氨基-5-吡唑基-1;3;4-噁二唑的合成及生物活性

关 键 词:取代氨基吡唑基噁二唑  2-取代氨基-5-吡唑基-1  4-噁二唑的合成及生物活性  
文章编号:1000-0518(2003)07-0624-05
收稿时间:2009-06-29
修稿时间:2002-12-04

Synthesis and Bioactivity of 2-Substituted amino-5-pyrazolyl-1,3,4-oxadiazoles
YUAN De-Kai,LI Zheng-Ming,ZHAO Wei-Guang,CHEN Han-Song. Synthesis and Bioactivity of 2-Substituted amino-5-pyrazolyl-1,3,4-oxadiazoles[J]. Chinese Journal of Applied Chemistry, 2003, 20(7): 624-628
Authors:YUAN De-Kai  LI Zheng-Ming  ZHAO Wei-Guang  CHEN Han-Song
Affiliation:YUAN De-Kai,LI Zheng-Ming*,ZHAO Wei-Guang,CHEN Han-Song
Abstract:Methylthio-5-pyrazolyl-1,3,4-oxadizole 1 was oxidized by KMnO 4/HAc to give 2-methylsulfonyl-5-pyrazolyl-1,3,4-oxadiazole 2. Nucleophilic reaction of 2 with arylamines afforded the title compounds 2-arylamino-5-pyrazolyl-1,3,4-oxadiazoles 3. Structures of 2 and 3 were determined by elemental analysis, 1H NMR and mass spectrometry. The MS fragmentation patterns of compounds 2A and 2B were discussed. Bioassay showed that at a mass fraction of 0.005%, 2A and 2B inhibited Phoma asparagi by 40% and 60%. Compound 3A-5 and 3B-1 also have certain fungicidal activity.
Keywords:methylsulfonyl-pyrazolyl-oxadiazole  synthesis  bioactivity
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