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6-氨基-3-取代吲哚的合成和生物活性研究 总被引:1,自引:0,他引:1
6-氨基-3-取代吲哚及其衍生物是一种重要的医药和有机化工中间体,不仅能合成一些具有生理活性和药理活性的化合物,如:合成一些具有药物活性的色胺类化合物及其衍生物[1,2];合成一些植物生长调节剂,如吲哚-3-乙腈和吲哚-3-乙酸类化合物[3];合成一些具有生物活性的天然化合物Drag 相似文献
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赛吲哚霉素的双乙酰衍生物已由吲哚瞒-吲哚法合成.吲哚-3-乙酸经催化氢化,甲酯化和氨解反应得到吲哚瞒-3-乙酰胺(9);将4-去氧-D-核-吡喃己糖以三苯甲基保护后乙酰化.消除保护基再经氧化和甲酯化等反应,得到1,2,3-O-三乙酰基-4-去氧-β-D-核-吡喃己糖醛酸甲酯(6),将化合物6和9先缩合后脱氢即得到赛吲哚霉素的双乙酰衍生物2.赛吲哚霉素的类似物1-(3-氨羰甲基吲哚基)-2,3,4,6-O-四乙酰基-β-D-吡喃葡萄糖苷(13)也由相似的方法合成. 相似文献
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1-苯基-3-(3'-吲哚基)-5-取代苯基-2-吡唑啉的合成及1H NMR和MS中的取代基效应 总被引:1,自引:0,他引:1
J-(3'-吲哚基)-3-取代苯基-2-丙烯-1-酮与茉肼反应,合成了10种新的1-苯基-3-(3'-吲哚基)-5-取代苯基-2-吡唑啉衍生物,其结构通过各种波谱证实.讨论了此系列化合物1HNMR和Ms中的取代基效应,得出取代基常数σ或σ+与质子化学位移,碎片相对丰度之间存在着良好的线性关系. 相似文献
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通过银促进的傅-克反应可以合成系列C3α-位为不同类型芳基取代的四氢吡咯并吲哚骨架的类天然产物.在该合成方法的基础上,发现C3α-位分别为对乙酰氨基苯基取代和甲基吲哚取代的四氢吡咯并吲哚类衍生物3a和3b对多种肿瘤细胞均表现出微摩尔级的活性,是具有重要临床应用前景的药物候选化合物.为了进一步研究该类化合物的成药性及其构效关系,以化合物3a为前体化合物合成了一系列类天然产物(化合物4~17),对其抗肿瘤活性进行了研究,并初步探讨了其构效关系.所合成化合物的结构经1H NMR、13C NMR和HRMS分析确证.本研究为该类化合物的临床前研究奠定了基础. 相似文献
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吲哚以其独特的化学结构使其衍生出的化合物都具有独特的生理活性,它们在医药、农药、香料、色氨酸等领域发挥着重要的作用,是一类非常重要的杂环类精细化工中间体。因此,长久以来发展简单、通用,特别是具有区域选择性的方法合成吲哚类化合物一直吸引了人们的研究兴趣[1]。在已经发展起来的合成吲哚类化合物的许多方法中,Heck反应[2],即Pd催化卤代物与烯烃构筑碳碳键的方法,由于其温和的反应条件和广泛的官能团相容性,已经成为合成吲哚及其衍生物采用最多的方法[3]。早在1984年,Suzuki[4]就报道合成了化合物3-乙氧羰基-2-甲基吲哚,其是由… 相似文献
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The reaction of indole and its derivatives with aryldiazoacetates has been studied in the presence of copper and rhodium catalysts. The electronic property of N-1 substitutent showed significant effect on the reaction pathways. The electron-donating group favored the formation of the β-alkylation products, while the electron-withdrawing group favored the formation of the cyclopropane products. A reaction mechanism was proposed based on the experimental data and previous research results. The structure of aryl group in diazo compounds also affected the yield of the β-alkylation products or the cyclopropane products. 相似文献
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ZENG Xiang-Chao② XU Shi-Hai LIU Po-Runa DENG Qin-Ying 《结构化学》2005,24(3):299-302
1 INTRODUCTION Indole and its derivatives have attracted much at-tention due to their chemical properties as well asbiological activities[1, . They have been widely used 2]as the materials for producing pigment, perfume,plant growth regulators, etc. Recently, it has alsobeen found that some indole derivatives present anti-tumor and antiviral activities[3~5]. During our sear-ches for bioactive compounds, a series of indole deri-vatives were synthesized, among … 相似文献
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Fischer吲哚合成法的研究进展 总被引:10,自引:0,他引:10
吲哚及其衍生物具有某些生物活性, 其合成方法很多. 其中Fischer吲哚合成是最便捷和经济的合成方法, 应用最多. 对此法近十年来的合成工艺进行了综述和评价. 相似文献
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Tryptophanase (Trpase) encoded by the tnaA gene catalyzes the conversion of tryptophan to indole, which is an extracellular signaling molecule detected in various bacteria including Vibrio cholerae. Indole has been demonstrated to regulate biofilm formation, drug resistance, plasmid maintenance and spore formation of bacteria. In the present study, the tnaA gene from V. cholerae O1 (VcTrpase) was cloned and expressed in E. coli BL21(DE3) tn5:tnaA (a Trpase-deficient competent). VcTrpase was purified by Ni2+-NTA chromatography. The obtained VcTrpase had a molecular mass of approximately 49 kDa, a specific activity of 3 U/mg protein, and absorption peaks at 330 and 435 nm. Using a site-directed mutagenesis technique, replacement of Arg419 by Val resulted in a VcTrpase completely devoid of activity. Thus, this site can be a target for drug design for controlling V. cholerae. 相似文献
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T. E. Khoshtariya L. N. Kurkovskaya K. T. Batsikadze M. M. Matnadze M. I. Sikharulidze V. O. Ananiashvili T. O. Dzhashi I. G. Abesadze M. G. Alapishvili 《Chemistry of Heterocyclic Compounds》2007,43(3):286-291
A new method is described for the synthesis of the heterocyclic systems of benzo[b]thiophenoindoles from the respective isomeric
amino acids with amino groups at positions 2 and 3. The method makes it possible to produce the tetracyclic systems with both
angular and linear structure. The classical Fischer reaction served as model for such transformations.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 3, pp. 361–367, March, 2007. 相似文献
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T. E. Khoshtariya L. N. Kurkovskaya M. M. Matnadze M. I. Sikharulidze V. O. Ananiashvili T. O. Dzhashi K. T. Batsikadze 《Chemistry of Heterocyclic Compounds》2007,43(10):1239-1246
A new method is described for the synthesis of the 1H-benzo[b]furoindole heterocyclic systems from the corresponding isomeric
amino acids with amino groups at positions 2 and 3. By this method it is possible to obtain these tetracyclic systems not
only in the form of one isomer but also to convert them from one to the other. From the tetracyclic systems with angular structure
it is possible to obtain the corresponding linear isomers. On the other hand, from the isomer with the linear structure it
is possible to change to the isomer with angular fusion of the pyrrole ring. The classical Fischer reaction served as model
for such transformations.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1463–1471, October, 2007. 相似文献
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Development of indole synthesis by tin-mediated radical cyclization of o-alkenylphenyl isocyanide is described. Upon heating o-alkenylphenyl isocyanide in the presence of tri-n-butyltin hydride and AIBN, 2-stannyl-3-substituted indole was formed via 5-exo-trig cyclization of the imidoyl radical intermediate. After acidic workup, 3-substituted indoles were isolated. For substrates bearing simple alkyl groups, a substantial amount of tetrahydroquinoline derivatives were generated through 6-endo-trig cyclization. This undesired cyclization was suppressed by using an excess amount (five equivalents based on o-alkenylphenyl isocyanide) of ethanethiol instead of tri-n-butyltin hydride. The 2-stannylindole intermediates proved to be a suitable substrate for Stille coupling, giving 2,3-disubstituted indoles in a one-pot procedure. In addition, the 2-stannylindole intermediates could be converted to 2-iodoindoles by treatment with iodine or N-iodosuccinimide. The 2-iodoindoles thus obtained served as good substrates for Heck reactions, Stille couplings, Suzuki couplings, and palladium-mediated carbonylations, to afford a variety of 2,3-disubstituted indoles. The utility of this protocol was demonstrated by application to synthetic studies on gelsemine and discorhabdin A, and the total synthesis of an aspidosperma alkaloid, (-)-vindoline. 相似文献
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开发了一种以吲哚为起始原料,合成具有多个反应位点的多取代3-烯基吲哚的新方法,合成了9个目标化合物,其中8个为新化合物,其结构经1H NMR, 13C NMR和HR-MS(ESI)表征。 相似文献
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William C. Neuhaus Ian J. Bakanas Joseph R. Lizza Charles T. Boon Jr. 《Green Chemistry Letters and Reviews》2016,9(1):39-43
Novel eco-friendly tetramethylguanidinium propanesulfonic acid trifluoromethylacetate ([TMGHPS][TFA]) ionic liquid was developed as catalyst and medium for the Fischer indole synthesis of a wide variety of hydrazines and ketones. The indole products were isolated in high yields and with minimal amounts of organic solvent. This reaction showed that [TMGHPS][TFA] can be regenerated and reused with reproducible yields without eroding the integrity of the ionic liquid. 相似文献