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吲哚二酮哌嗪类化合物是一类重要的杂环化合物,自然界中存在许多含有此结构单元的物质.由于该类物质具有多种生物活性,特别是抗肿瘤活性,因此它们的合成得到了广泛的研究.综述了吲哚二酮哌嗪类化合物的主要合成方法及其研究进展. 相似文献
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吲哚-2,3-二酮是一种广泛存在于天然产物中的化合物,基于其结构特点可以发生不同类型的反应,为其衍生物的合成提供了便利的条件,因此目前其合成和活性的研究备受关注.本文对近年来吲哚-2,3-二酮衍生物抗病毒活性研究情况进行了综述,分别介绍了对HIV、痘病毒、SARS病毒、柯萨奇病毒B3和烟草花叶病毒的抑制活性.重点介绍了吲哚-2,3-二酮衍生物对HIV病毒的作用以及对HIV病毒进入人体破坏人体的免疫功能后容易感染的细菌和结核病的作用. 相似文献
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以苯胺和氯乙酰氯为原料在NaOH存在下酰化合成N-氯乙酰基苯胺,然后N-氯乙酰基苯胺在无水AICI,催化下环化合成2-吲哚酮.对由N-氯乙酰基苯胺合成2-吲哚酮的工艺条件进行了改进.结果表明合成2-吲哚酮的最佳条件为:反应温度为220℃,反应时间为60min,加料时温度为180℃,N-氯乙酰基苯胺与氯化钠,无水AlCl3的重量比为1:1:5.5.改进后的合成2-吲哚酮收率达到88.3%,纯度99%,收率比原工艺提高了24.6%.在此基础上,还合成了5-甲基-2-吲哚酮,并得到其最佳条件为:反应温度为190℃,反应时间为30min,加料时温度为180℃,4-甲基-N-氯乙酰基苯胺与氯化钠,无水AlCl3的重量比为1:1:5.5,收率达到83.1%,纯度为99%. 相似文献
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Eu(NTf2)3催化吲哚与醛(酮)反应合成二吲哚基甲烷 总被引:3,自引:0,他引:3
二(三氟甲基磺酰)亚胺铕(Ⅲ)[Eu(NTf2)3,Tf=SO2CF3]作催化剂,吲哚与醛(酮)在室温下发生亲电取代反应合成了一系列二吲哚基甲烷,产率85%~98%.该法反应条件温和、时间短、催化剂用量少且可以回收重复使用. 相似文献
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以苯胺为原料,通过肟化、环合生成二氢吲哚-2,3-二酮,再对其进行N-烷基化、亲核加成和磺酰化反应得到目标化合物5a~5g和7a~7e。通过1H NMR、13C NMR确认其结构。采用噻唑蓝(MTT)法测试了目标化合物对乳腺癌细胞MDA-MB-231、鼠黑色素瘤细胞B16、鼠结肠癌细胞CT26三种肿瘤细胞的体外抑制活性。结果表明,化合物7d、7e具有明显的肿瘤细胞毒活性,其中化合物7d对MDA-MB-231的细胞毒活性比阳性药五氟尿嘧啶更强,IC50为4.63±0.14μmol/L。本文结果可为进一步研究具有肿瘤细胞毒活性的吲哚酮类衍生物提供参考。 相似文献
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以苯胺为原料,通过传统方法合成靛红。靛红与盐酸羟胺反应生成3-羟基亚氨基-2-吲哚酮,再通过钯碳加氢还原生成3-氨基-2-吲哚酮。合成中,采用钯碳加氢的还原方式,产物收率提高(收率82.76%,较文献提高了11.8%),后处理更简单,而且该方法可操作性高,成本低,产生三废少,是一条适合大规模生产3-氨基-2-吲哚酮的新合成工艺路线。 相似文献
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Carbonyl-containing oxindoles are ubiquitous core structures present in many biologically active natural products and pharmaceutical molecules. Nickel-catalyzed reductive aryl-acylation of alkenes using aryl anhydrides or alkanoyl chlorides as acyl sources is developed, providing 3,3-disubstituted oxindoles bearing ketone functionality at the 3-position. Moreover, nickel-catalyzed reductive aryl-esterification of alkenes using chloroformate as ester sources is further developed, affording 3,3-disubstituted oxindoles bearing ester functionality at the 3-position. This strategy has the advantages of good yields and high functional group compatibility. 相似文献
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A highly regio‐, diastereo‐, and enantioselective allylic alkylation reaction of 3‐monosubstituted oxindoles catalyzed by molybdenum is described. The reaction is affected by the electronic and steric variations of the nucleophile. The use of appropriate N‐protecting group is particularly important for achieving high regio‐ and diastereoselectivity. Products from this reaction, containing vicinal quaternary‐tertiary stereogenic centers, are valuable synthetic intermediates and should find utility in alkaloid synthesis. 相似文献
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Highly Enantioselective Tandem Michael Addition of Tryptamine‐Derived Oxindoles to Alkynones: Concise Synthesis of Strychnos Alkaloids 下载免费PDF全文
Weigang He Jiadong Hu Pengyan Wang Le Chen Kai Ji Siyu Yang Yin Li Zhilong Xie Prof. Dr. Weiqing Xie 《Angewandte Chemie (International ed. in English)》2018,57(14):3806-3809
A highly enantioselective tandem Michael addition of tryptamine‐derived oxindoles to alkynones was developed by taking advantage of a chiral N,N′‐dioxide Sc(OTf)3 catalyst. The reaction enables the facile preparation of enantioenriched spiro[pyrrolidine‐3,3′‐oxindole] compounds, which provides a novel strategy for the synthesis of monoterpenoid indole alkaloids. As a demonstration, the asymmetric synthesis of strychnos alkaloids [(?)‐tubifoline, (?)‐tubifolidine, (?)‐dehydrotubifoline] was achieved in 10–11 steps. 相似文献
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过渡金属催化的烯丙基取代反应是一类重要且实用的有机化学反应, 可以立体选择性地高效构建碳-碳键和碳-杂键. 可见光氧化还原催化可以利用绿色清洁的可见光能源在较为温和的条件下产生自由基或者自由基离子等高反应活性的反应中间体, 被广泛地应用于有机合成中, 逐渐发展成为一种重要的合成工具. 鉴于烯丙基取代反应的重要性, 过渡金属与光氧化还原协同催化的烯丙基取代反应逐渐引起化学家的兴趣. 该协同催化的策略可以实现单一过渡金属催化难以实现的烯丙基取代反应, 反应的区域选择性和立体选择性也体现出不同的特点, 有望发展成为单一金属催化的烯丙基取代反应的重要补充. 本文综述了近年来不同过渡金属与可见光氧化还原协同催化的烯丙基取代反应的研究进展. 相似文献
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发展了一种可见光诱导的共轭磺酰胺串联脱砜/环化,合成全氟烷基化吲哚酮或α-芳基酰胺的方法。此反应以多氟烷基碘或溴为氟源,在发光二极管蓝光灯照射下,利用面式-三(2-苯基吡啶)合铱催化N-烷基-N-甲基丙烯酰基苯磺酰胺经过串联自由基加成/β-芳基迁移/脱砜环化过程,一步构筑两重碳-碳键,以41%~78%的产率合成了一系列含氟吲哚酮或α-芳基酰胺。此方法底物适用范围广,反应条件温和(室温),催化体系绿色,为具有潜在生理活性的含氟吲哚酮及α-芳基酰胺的合成提供了一条高效、快捷的新途径。 相似文献
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Xiaodong Shen Dr. Klaus Harms Michael Marsch Prof. Dr. Eric Meggers 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(27):9102-9105
A bis‐cyclometalated rhodium(III) complex catalyzes a visible‐light‐activated enantioselective α‐amination of 2‐acyl imidazoles with up to 99 % yield and 98 % ee. The rhodium catalyst is ascribed a dual function as a chiral Lewis acid and, simultaneously, as a light‐activated smart initiator of a radical‐chain process through intermediate aminyl radicals. Notably, related iridium‐based photoredox catalysts reported before were unsuccessful in this enantioselective radical C?N bond formation. The surprising preference for rhodium over iridium is attributed to much faster ligand‐exchange kinetics of the rhodium complexes involved in the catalytic cycle, which is crucial to keep pace with the highly reactive and thus short‐lived nitrogen‐centered radical intermediate. 相似文献
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Dr. Dmitry Katayev Prof. Yi‐Xia Jia Akhilesh K. Sharma Dr. Dipshikha Banerjee Dr. Céline Besnard Prof. Raghavan B. Sunoj Prof. E. Peter Kündig 《Chemistry (Weinheim an der Bergstrasse, Germany)》2013,19(36):11916-11927
Palladium complexes incorporating chiral N‐heterocyclic carbene (NHC) ligands catalyze the asymmetric intramolecular α‐arylation of amides producing 3,3‐disubstituted oxindoles. Comprehensive DFT studies have been performed to gain insight into the mechanism of this transformation. Oxidative addition is shown to be rate‐determining and reductive elimination to be enantioselectivity‐determining. The synthesis of seven new NHC ligands is detailed and their performance is compared. One of them, L8 , containing a tBu and a 1‐naphthyl group at the stereogenic centre, proved superior and was very efficient in the asymmetric synthesis of fifteen new spiro‐oxindoles and three azaspiro‐oxindoles often in high yields (up to 99 %) and enantioselectivities (up to 97 % ee; ee=enantiomeric excess). Three palladacycle intermediates resulting from the oxidative addition of [Pd(NHC)] into the aryl halide bond were isolated and structurally characterized (X‐ray). Using these intermediates as catalysts showed alkene additives to play an important role in increasing turnover number and frequency. 相似文献