苯並噻嗪及硫色滿衍生物的合成

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2015

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本論文分兩個部分 第一部分是利用硫代乙酸乙酯對二聚體苯並噻嗪進行親核取代反應,可得不同取代基且具有高度生物活性潛力的三聚體苯並噻嗪。有鑑於苯並噻嗪是許多藥物的結構單元,期望本方法對未來合成應用上有所幫助。 第二部分將硫代乙酸乙酯和硝基苯乙烯衍生物,以丙酮當溶劑於室溫下反應,藉由4-二甲氨吡啶(DMAP)的催化下,進行1.4-加成反應,生成硫色滿衍生物。此合成策略是利用較簡單且溫和的條件合成結構較複雜的硫色滿衍生物。
The contents of this dissertation is divided into two parts summarizing the results based on the experimental works performed during the course of study. The first part is about the syntheses potential bioactive compounds such as benzothiazine derivatives from (2-formylphenyl) ethanethioate and dimer benzothiazine through a nucleophilic substitution reaction. In the second part, we developed an efficient method for the synthesis of thiochroman derivatives via DMAP catalyzed one pot reaction of (2-formylphenyl) ethanethioate and nitrostyrene derivatives in acetone at room temperature. The procedure is simple and mild condition to obtain the highly substituted thiochroman derivatives.

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苯並噻嗪, 硫色滿, 生物活性, 親核取代反應, 麥可反應, benzothiazine, thiochroman, nucleophilic substitution, Michael reaction, bioactive

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