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根据活性亚结构拼接原理,将3-芳基-4-氨基-5-乙氧羰基(氰基)-3H-噻唑啉-2-硫酮与酰氯反应得到目标化合物3-芳基-4-取代苯氧乙酰氨基-5-乙氧羰基(氰基)-3H-噻唑啉-2-硫酮.再以3-苯基-4-氨基-5-乙氧羰基-3H-噻唑啉-2-硫酮为合成原料,经过Aza-Wittig反应得到目标化合物5-芳氧基-3,6-二芳基-2-硫代噻唑并[4,5-d]嘧啶-7-酮.通过IR,1H NMR,EI-MS,元素分析等方法对所合成的化合物进行了结构表征.代表化合物5-对氯苯氧基-3,6-二苯基-2-硫代-2,3-二氢噻唑并[4,5-d]嘧啶-7(6H)-酮(C1)经单晶X衍射证实了结构.除草活性测试结果表明:部分噻唑啉-2-酮类衍生物对稗草和油菜都表现出了较好的抑制活性.
The 3-aryl-4-amino-5-ethoxycarbonyl (cyano) -3H-thiazoline-2-thione is reacted with an acid chloride according to the principle of active substructure to obtain the target compound 3-aryl-4-substituted Phenoxyacetamido-5-ethoxycarbonyl (cyano) -3H-thiazoline-2-thione, and then 3-phenyl-4-amino-5-ethoxycarbonyl-3H-thiazoline-2- Ketone as the starting material, the target compound 5-aryloxy-3,6-diaryl-2-thiazolo [4,5-d] pyrimidin-7-one was obtained by Aza- Wittig reaction. NMR, EI-MS, elemental analysis, etc. The representative compounds 5-p-chlorophenoxy-3,6-diphenyl-2-thio-2,3-dihydrothiazole The structure of [4,5-d] pyrimidin-7 (6H) -one (C1) was confirmed by single crystal X-ray diffraction.The results of herbicidal activity test showed that some thiazolin- Showed better inhibitory activity.