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The fully substituted cyclopentenedione core of madindoline A (1) and B (2) as potent and selective inhibitor of IL-6 has been synthesized efficiently. The quaternary carbon center C-2' was constructed on the basis of a newly developed AIEt3-promoted tandem reductive rearrangement of α-hydroxy epoxides. 相似文献
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Introduction Diastereoselective construction of 1,3-diheteroatom units, especially 1,3-amino alcohols and 1,3-diols, has always been in high demands in synthetic organic chemistry, as they are widely present in many natural products and potent drugs, such as nucleoside antibiot-ics and the HIV protease inhibitors.1,2 They have also been used as chiral ligands for asymmetric catalysts and as synthetic intermediates.3 Although several methods for the construction of 1,3-amino alcohols have been… 相似文献
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Michael加成反应和Aldol反应是有机合成中最基本和最常见的两种反应类型.通过对反应条件的调控和底物的设计,使卤素离子(Cl~—,Br~—,I~—)对α,β-不饱和化合物发生Michael加成之后,生成的活性中间体与醛在同一体系中继续进行Aldol反应得到多官能团产物,这一反应被称为halo-Michael/Aldol串联反应.Halo-Michael/Aldol串联反应可以有效提高有机合成的原子经济性和步骤经济性.总结了不同类型路易斯酸促进的halo-Michael/Aldol串联反应及其在合成中的应用,并展望了该反应的发展趋势. 相似文献
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萜类化合物在自然界中广泛存在,其中倍半萜内酯广泛存在于各种药用植物中,是许多传统中草药的主要活性成分,然而这类化合物的化学全合成却极具挑战性.山道年是一种廉价的可再生资源,且光促进的山道年重排反应是一种构建愈创木内酯骨架的高效方法,在萜类天然产物合成中得到广泛应用.就光促进的山道年重排在复杂萜类天然产物的合成工作进行简单的概述,主要包括倍半萜内酯及其寡聚物全合成以及个别二萜天然产物的骨架合成研究. 相似文献
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<正>天然产物全合成是有机化学中的重要研究领域,其持续不断发展为创新药物的发现提供了重要的保证.其中,约一半新发现的小分子药物都来源于天然产物及其衍生物[1].由于天然产物结构复杂,含量稀少且难以通过分离手段来获得稳定来源,极大地限制了天然产物在药物研发中的应用.合成方法与策略的创新,对推动天然产物全合成领域的发展起着非常关键的作用.值得注意的是,利用分子内的Pauson-Khand反应在合成具有环戊烯酮骨架的天然产物中扮演着重要角色[2]. 相似文献
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A facile and highly diastereoselective method for the construction of 2-quaternary 1,3-amino alcohols and 1,3-diols has been developed on the basis of the AlEt3/THF-promoted tandem rearrangement/reductive reaction of α-hydroxy (amino) aziridines (epoxides). The progressive achievement in this article included that both 2-epimers of the units could be constructed from the initially same substrate. Also a stereochemistry assignment we reported previously was corrected. 相似文献
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