發(fā)布時間：2018-04-11 14:19

  本文選題：喜樹堿 + 全合成　； 參考：《華東師范大學(xué)》2017年碩士論文

【摘要】：本論文主要是研究氫胺化-內(nèi)酰胺化串聯(lián)反應(yīng)在天然產(chǎn)物及其類似物合成中的應(yīng)用,包括以下兩個部分:第一部分:喜樹堿類似物的合成研究在前期研究的基礎(chǔ)上,我們通過合理的設(shè)計,探索并優(yōu)化了氫胺化-內(nèi)酰胺化串聯(lián)環(huán)化反應(yīng)條件,并將其應(yīng)用于喜樹堿類似物的合成中。在內(nèi)酯片段引入炔烴,通過Sonogashira偶聯(lián)反應(yīng)得到串聯(lián)環(huán)化前體化合物,應(yīng)用串聯(lián)環(huán)化反應(yīng),完成了1個新型喜樹堿類似物的合成。第二部分:烏檀屬生物堿的全合成研究應(yīng)用氫胺化-內(nèi)酰胺化串聯(lián)環(huán)化反應(yīng),對吲哚吡啶類生物堿進(jìn)行集體合成,同時進(jìn)一步考察氫胺化-內(nèi)酰胺化串聯(lián)環(huán)化反應(yīng)的底物普適性。最終以良好到優(yōu)秀的收率完成了天然產(chǎn)物angustidine,neonaucline以及類似物20-bromonauclefine的全合成,并對這些天然產(chǎn)物及其類似物進(jìn)行生物活性測試。
[Abstract]:This thesis mainly studies the application of series reaction of hydroamination and lactam in the synthesis of natural products and their analogues, including the following two parts: the first part: the synthesis of camptothecin analogues is based on the previous studies.Through reasonable design, we have explored and optimized the reaction conditions of series cyclization of hydroamination and lactam, and applied them to the synthesis of camptothecin analogues.A novel camptothecin analogue was synthesized by introducing alkynes into lactone segment and Sonogashira coupling reaction to obtain series cyclized precursor compounds.The second part: the total synthesis of alkaloids of the genus Acetanthus; the synthesis of indolopyridine alkaloids by series cyclization of hydroamination and lactam was carried out.At the same time, the substrate universality of hydroamination-lactam series cyclization reaction was also investigated.Finally, the complete synthesis of natural product angustidine neonaucline and its analogues 20-bromonauclefine was completed with excellent yield, and the bioactivity of these natural products and their analogues was tested.
【學(xué)位授予單位】：華東師范大學(xué)
【學(xué)位級別】：碩士
【學(xué)位授予年份】：2017
【分類號】：O629
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本文編號：1736350