首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and molluscicidal activity of some new thiophene, thiadiazole and pyrazole derivatives.
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Synthesis and molluscicidal activity of some new thiophene, thiadiazole and pyrazole derivatives.

机译:一些新的噻吩,噻二唑和吡唑衍生物的合成和杀灭软体动物的活性。

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摘要

The base-catalyzed reaction of benzoyl acetone 1 with phenyl isothiocyanate yields the non-isolable intermediate 2. Treatment of 2 with dilute HCl afforded the corresponding thiocarbamoyl derivative 3. Reaction of the intermediate 2 with phenacyl bromide, ethyl bromoacetate, chloroacetonitrile, chloroacetyl chloride, bromodiethyl malonate and chloroacetone afforded the corresponding thiophene derivatives 5, 8, 15 and 17. The thiocarbamoyl derivative 3 reacts with arylazophenacyl bromide and/or hydrazine hydrate to afford the corresponding thiadiazole and pyrazole derivatives 20a-c and 22, respectively. These new synthesized compounds show generally a moderate molluscicidal activity to Biomphalaria alexandrina snails.
机译:苯甲酰基丙酮1与异硫氰酸苯酯的碱催化反应生成不可分离的中间体2。用稀HCl处理2得到相应的硫代氨基甲酰基衍生物3。中间体2与苯甲酰溴,溴乙酸乙酯,氯乙腈,氯乙酰氯,丙二酸溴二乙酯和氯丙酮分别提供相应的噻吩衍生物5、8、15和17。硫代氨基甲酰基衍生物3与芳基偶氮苯甲基溴化物和/或水合肼反应,分别得到相应的噻二唑和吡唑衍生物20a-c和22。这些新合成的化合物通常对亚历山大草(Biomphalaria alexandrina)蜗牛具有中等的杀软体动物活性。

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