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青蒿素以其突出的抗疟活性和特殊的1,2,4-三(口恶)烷结构引起了国内外药学和化学工作者的广泛兴趣。合成并考察类似结构的化合物是探索青蒿素构效关系和发展新型药物的一个重要途径,本文报道用臭氧化方法探索合成青蒿素类似物的一些结果。近年来我们曾研究并报道了一些青蒿素的降解反应,降解产物尤其是双酮甲酯Ⅰ产率高,且具有与青蒿素相应的构型,因此是合适的接力中间体,由此既可用于重组青蒿素本身,也可用于合
Artemisinin has attracted a great deal of interest from pharmaceutical and chemical workers at home and abroad for its outstanding antimalarial activity and its unique 1,2,4-trioxane structure. The synthesis and investigation of compounds of similar structure is an important way to explore the structure-activity relationship of artemisinin and the development of new drugs. Some results of the synthesis of artemisinin analogues by ozonation are reported here. In recent years we have studied and reported on the degradation reaction of some artemisinins. The degradation products, especially diketophenylal I, have high yields and have the configuration corresponding to artemisinin and are therefore suitable relay intermediates Can be used to recombine artemisinin itself, can also be used together