含1,3,4-噻二唑环吡唑并[3,4-d]嘧啶类化合物的合成及生物活性

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通过5-氨基-4-氰基-1-苯基吡唑与甲酸发生环合、再经氯化和芳香族亲核取代反应,合成了12种新的含1,3,4-噻二唑环吡唑并[3,4-d]嘧啶类化合物.目标化合物的结构经红外光谱、核磁共振氢谱、质谱和元素分析方法予以确认.初步的生物活性测定试验表明,在50 mg/L浓度下,大部分目标化合物对小麦纹枯病菌(Rhizoctonia cerealis)表现出较好的杀菌活性,其中化合物5b,5d和5j的抑菌率超过90%. Through the ring-closure of 5-amino-4-cyano-1-phenylpyrazole with formic acid and subsequent chlorination and aromatic nucleophilic substitution reactions, 12 new 1,3,4-thiadiazoles Cyclopyrazolo [3,4-d] pyrimidines were synthesized.The structures of target compounds were confirmed by IR, 1HNMR, MS and elemental analysis.A preliminary bioassay assay showed that under the concentration of 50 mg / L , Most of the target compounds showed good bactericidal activity against Rhizoctonia cerealis, and the inhibitory rates of compounds 5b, 5d and 5j exceeded 90%.
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