取代吡唑并[4,5-e][1,3]噻嗪衍生物的合成及生物活性
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF SUBSTITUTED PYRAZOLO [4,5 e][1,3]THIAZINE DERIVATIVES
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摘要: 取代吡唑酰基异硫氰酸酯与杂环胺、磺酰胺反应 ,得到了加成产物取代吡唑酰基硫脲或关环产物吡唑并 [4 ,5- e][1,3]噻嗪。取代吡唑酰基硫脲化合物在三乙胺作用下也关环成吡唑并 [4 ,5- e][1,3]噻嗪。化合物结构均经 1HNMR、IR及元素分析确证 ,并对此加成、环化反应结果和机理进行了讨论。初步生物活性测试表明 ,这些化合物具有一定的杀菌、除草和植物生长调节作用。Abstract: The additive compounds substituted pyrazolyl thiourea (II) or cyclic pyrazolo [4,5 e][1,3]thiazines (III) were obtained by reaction of heterocyclic (sulfonyl) amines with substituted pyrazolyl isothiocyanates. Compounds (II) were cyclized in the presence of triethylamine to give compounds (III) respectively. The structures of compounds (II) and (III) were conformed by 1H NMR, IR, MS and elemental analysis and the reaction results were discussed. The preliminary bioassay presented that some of compounds showed fungicidal, herbicidal and plant growth regulatory activities.
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Key words:
- pyrazolyl thiourea /
- thiazine /
- addition /
- cyclization /
- biological activity
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Stet ter J. , A lig B. , M arho ld A. , et al. , Ger. O ffen. DE 4, 414, 333,CA 1996, 124: 87008j H irohara Yiji, N akajima H idek i, Kash iw abara Takash i, et al. , Jpn. Kokai Tokkyo Koho JP10158, 107,CA 1998, 129: 41127x Zagar C. , Hamp rech t G. , M engesM. et al. , PCT Int. App l. WO 9838169, CA 1998, 129: 216614a 金桂玉, 侯震, 赵国锋等, 高等学校化学学报, 1997, 18: 409 -
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