Citation:
ZHANG Xiu-Li, LÜ Xian-Hai, JIANG Wan-Quan. Synthesis and Fungicidal Activity of New Pyrazole-Acyl Fluoro-Substituted Aromatic Thiourea Derivatives[J]. Chinese Journal of Applied Chemistry,
;2008, 25(4): 459-463.
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Nine novel pyrazole-acyl fluoro-substituted aromatic thiourea derivatives were synthesized from phenylhydrazine and ethyl acetoacetate.The intermediate 4 was prepared via a series of reactions involving cyclization,formylation,oxidation and acylation,and was subsequently reacted with amonium thiocyanate to generate the corresponding intermediate 5 with good yield in the presence of phase transfer catalyst PEG-600.The obtained intermidiate 5 was then reacted with fluoro-substituted anilines to form the desired pyrazole-acyl fluoro-substituted aromatic thiourea derivatives,and their structures were identified by IR,1H NMR and elemental analysis.Preliminary bioassays indicated that compounds 6a,6b,6d,6e,6f,6g,6h and 6i showed inhibitory activities (100%) against Rhizoctonia sasakii,and compound 6e showed inhibitory activities (98.2%) against Gibberella zeae at a concentration of 50 mg/L.
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