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首页> 外文期刊>Zeitschrift fur Naturforschung, B. A Journal of Chemical Sciences >Synthesis of Pyrimidine, Thiazolopyrimidine, Pyrimidotriazine and Triazolopyrimidine Derivatives and their Biological Evaluation
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Synthesis of Pyrimidine, Thiazolopyrimidine, Pyrimidotriazine and Triazolopyrimidine Derivatives and their Biological Evaluation

机译：嘧啶，噻唑并嘧啶，嘧啶三嗪和三唑并嘧啶衍生物的合成及其生物学评价

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摘要

Pyrimidin-4-one-2-thione (3) was synthesized via the reaction of thiourea (1) with ethyl benzoylacetate (2) and was taken as a starting material for the present study via its reactions with the halogen-containing reagents 4a-d and 10a-c to give the corresponding thiazolopyrimidines 8, 9 and 12a-c. The 2-hydrazino derivatives 4 were synthesized either via the reaction of 3 or 4 with hydrazine hydrate. Compound 4 reacted with 4a-c and 10a-c to give the corresponding pyrimidotriazines 17a-c and 19 and 19 respectively. Also, compound 4 reacted with the active methylene-containing reagents 13 and 2a, b to give the corresponding 2-pyrazolopyrimidines 15 and 22a, b respectively. On the other hand, the triazolopyrimidines 21a, b and 30a, b were also obtained via the reaction of 5 with each of formic acid, acetic anhydride, ethyl chloroformate and carbon disulfide respectively. Some of the newly synthesized heterocyclic derivatives were tested for their biological activity.
机译：通过硫脲（1）与苯甲酰乙酸乙酯（2）的反应合成了嘧啶-4-一-2-硫酮（3），并通过与含卤素试剂4a-的反应作为本研究的原料d和10a-c给出相应的噻唑并嘧啶8、9和12a-c。通过3或4与水合肼的反应合成2-肼基衍生物4。化合物4与4a-c和10a-c反应，分别得到相应的嘧啶三嗪17a-c和19和19。同样，化合物4与活性的含亚甲基的试剂13和2a，b反应，分别得到相应的2-吡唑并嘧啶15和22a，b。另一方面，三唑并嘧啶21a，b和30a，b也分别通过5与甲酸，乙酸酐，氯甲酸乙酯和二硫化碳的反应获得。测试了一些新合成的杂环衍生物的生物活性。

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