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氨基香豆素类抗生素系一类兼具细菌DNA解旋酶B(DNA gyrase B)和人体热休克蛋白90(Hsp90)抑制活性的天然产物。因缺乏有效的合成手段,有关此类化合物的构效关系信息非常有限。本文首次详细探讨了3-O-酰化L-诺维糖的从头合成方法,并最后完成了一系列4-去羟基氯新生霉素类似物的合成,为氨基香豆素类化合物的合成提供了一套可行的化学合成路线。该路线的扩展应用将有助于氨基香豆素类化合物构效关系研究的进一步深入。
Aminocoumarins are natural products that combine both bacterial gyrase B and human Hsp90 inhibitory activity. Due to the lack of effective synthesis means, the structure-activity relationship information of these compounds is very limited. In this paper, the de novo synthesis of 3-O-acylated L-Nouveaura is discussed in detail for the first time. Finally, a series of 4-dehydroxychloroxybemycin analogues are synthesized and provided for the synthesis of aminocoumarins A viable chemical synthesis route. The extended application of this route will help to further study the structure-activity relationship of aminocoumarins.