Citation:
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.
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2-Methylthio-5-pyrazolyl-1,3,4-oxadizole 1 was oxidized by KMnO4/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.
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Keywords:
- methylsulfonyl-pyrazolyl-oxadiazole,
- synthesis,
- bioactivity
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