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Triethylborane promotes the Pd-catalyzed allylic alkylation of a wide variety of indoles with 1,3-butadiene to provide C3-octadienylindoles and C3-bis(octadienyl)indolenines in good to excellent yields under mild conditions.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Experimental anf theoretical studies on the acidity and basicity of a representative set of benzene substituted indoles have been carried out.Aqueous ionization data, obtained spectrophotometrically at 25 deg C, were comparatively analyzed by the Hammett Acidity function and the Excess Acidity methods.Ionization constants, pKas and solvation m* parameters are reported.Gas-phase ionization enthalpies have been theoretical calculated using the AM1 semiempirical method.Single and double parameter relationships between the theoretical and experimental ionization data and the Hammett substituent constants are observed.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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A mild and efficient iodine-catalyzed direct substitution of hydroxy group of allylic, progargylic and other alcohols with various C- and N-nucleophiles was described in this contribution. C-C and C-N bond formations could be readily achieved by non-metallic and green catalysis for various compounds. This facilitates access to possible transformations of a broad scope of substrates into bioactive and pharmaceutically important building blocks.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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A novel series of C12 vinyl erythromycin derivatives have been discovered which exhibit in vitro and in vivo potency against key respiratory pathogens. The C12 modification involves replacing the natural C 12 methyl group in the erythromycin core with a vinyl group via chemical synthesis. From the C12 vinyl macrolide core, a series of C12 vinyl ketolides was prepared. Several compounds were found to be potent against macrolide-sensitive and -resistant bacteria. The C12 vinyl ketolides 6j and 6k showed a similar antimicrobial spectrum and comparable activity to the commercial ketolide telithromycin. However, the pharmacokinetic profiles of C12 vinyl ketolides 6j and 6k in rats differ from that of telithromycin by having higher lung-to-plasma ratios, larger volumes of distribution, and longer half-lives. These pharmacokinetic differences have a pharmacodynamic effect as both 6j and 6k exhibited better in vivo efficacy than telithromycin in rat lung infection models against Streptococcus pneumoniae and Haemophilus influenzae.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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A gold-catalyzed method for the construction of indolizines with eight-membered rings has been developed. The reaction proceeded through a two-fold hydroarylation with indole or pyrrole derivatives containing a 1,6-diyne using a tri(1-adamantyl)phosphine gold complex as the catalyst, affording 1,8-disubstituted indolizines in moderate to good yields in DCE at 80 C. The potential usefulness of these indolizines as blue or green OLEDs has been also disclosed.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Archives for Chemistry Experiments of 4-Nitroindole

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The present invention discloses a pharmaceutical intermediate 4 – nitro indole preparation method, specifically comprises the following steps: first to methyl benzene sulfonic acid, citric acid, cerium nitrate as the raw material, and by the reaction of the alkaline solution containing the methyl benzene sulfonic acid, citric acid of cerium complex compositions, then taking it as catalyst catalytic 2 – methyl – 3 – nitroaniline and original carboxylic acid triethyl phosphite to make N – (2 – methyl – 3 – nitrophenyl) b oxygen radical armor imine, finally it with diethyl oxalate, potassium acetate to obtain the target product. The method of the invention mild reaction conditions, the prepared yield of the object product. (by machine translation)

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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This work investigated the in vitro and in vivo anti-angiogenic activity of some pyrroloazaflavones, exactly 2-phenyl-1H-pyrrolo[2,3-h]quinolin-4(7H)ones, with vinblastine as reference compound. Growth inhibitory activity, migration, and capillary-like structures formation were determined in human umbilical vein endothelial cell cultures, and Matrigel plug assay was carried out to evaluate in vivo effects on angiogenesis. Collectively, our results indicate that some pyrroloazaflavone derivatives, at non-cytotoxic concentrations and like vinblastine are able: (i) to exert in vitro anti-angiogenic activity and (ii) to counteract in vitro and in vivo the pro-angiogenic effects of fibroblast growth factor-2 (FGF-2).

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Probes and methods are provided for detection and analysis of nucleic acid sequences. The probes are single-labeled oligonucleotide probes whose fluorescence emission changes in response to probe-target hybridization and dissociation. The methods are for analyzing one or multiple nucleic acid loci using the probes. This invention further relates to the use of fluorescence changes in single-labeled probes for melting curve analysis, genotyping, and pathogen detection, and to methods for quantification of specific sequences in real-time monitoring of nucleic acid amplification.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Indoles undergo smooth coupling with phenylacetylene in the presence of 10 mol % of gallium(III) chloride or gallium(III) bromide under mild conditions to afford the corresponding 1,1-bis(1H-3-indolyl)-1-phenylethanes.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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A mild and efficient allylation of indoles and amides in the presence of a catalytic amount of Amberlyst-15 has been described in this context. The recyclable heterogeneous catalytic system is practical and facile for the synthesis of C- and N-allylated derivatives and would be of importance for the development of the accordingly functional complex molecules. Copyright Taylor & Francis Group, LLC.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles