- Preparation method of 3-substituted oxidized indole and derivative
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The invention belongs to the technical field of organic chemistry and pharmaceutical chemistry and particularly relates to a method of preparing 3-substituted oxidized indole and a derivative. In themethod, with a 3-substituted indole derivative as a raw material and one or more of a tetrabutyl ammonium halide compound/sodium chloride/sodium iodide/potassium iodide as additives, and one or more of dichloromethane/1,2-dichloroethane/tetrahydrofurane/methylbenzene/1,4-dioxane/ethyl acetate/methanol are added as solvents; then one or more of [bis(trifluoroacetoxyl)iodine]benzene/iodosobenzene diacetate are added as oxidants in order to carry out a reaction with reaction temperature being controlled, thus producing the 3-substituted oxidized indole derivative. The method has gentle reaction conditions, simple operations, short reaction time and high yield, and is free of a metal catalyst and is environment-friendly.
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Paragraph 0056; 0058; 0131
(2018/06/26)
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- A novel and efficient method for the synthesis of 1 H -indol-3-yl acetates
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A catalyst-free method for the synthesis of 1H-indol-3-yl acetates from 1H-indoles is described. The reaction takes place in the presence of (diacetoxyiodo)benzene (DIB) and potassium hydroxide as the base under mild conditions (MeCN, 35°C, 1.5 h). This represents a simple and efficient new method for 1H-indol-3-yl acetate synthesis.
- Liu, Kexin,Wen, Ping,Liu, Jin,Huang, Guosheng
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experimental part
p. 3623 - 3626
(2010/12/20)
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- COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5HT6 receptor which are of the formula (I), wherein R1-R3 A, B, D, E, G, Q, and x are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 112
(2010/11/28)
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- Metal Reagents in Organic Reactions. Part-VI 1,2. Oxidation of Indoles with Thallium(III) Acetate
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The action of thallium(III) acetate on a number of indoles, differently substituted in the 2- and 3-positions, has been investigated. Monomeric and 'dimeric' oxidation products are obtained; the structures of the products depend on the substituents present in the substrate. A novel oxidative dimerisation of 2,3-disubstituted indoles to indolo[3,2-b]carbazoles is observed. The generation of the products could be rationalised by the initial formation of an unstable, non-isolable 3-thallated-indolenine derivative.
- Banerji, Avijit,Ray, Rita,Pal, Sudhir C.,Banerji, Debasis,Maiti, Kaustabh K.
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p. 698 - 704
(2007/10/03)
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- Kinetic Study of the Nitrosation of 3-Substituted Indoles
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Kinetic studies of the nitrosation reaction of three 3-substituted indoles (3-methylindole, indol-3-yl acetate and indole-3-acetic acid) show that the final state is an equilibrium between the reactants (nitrous acid and indole derivative) and the 1-nitroso derivative.Values of the rate constants for the nitrosation of the three indoles and denitrosation of the corresponding nitrosoindoles as well as values of the equilibrium constants have been obtained.The almost complete insensitivity of the reaction rates to medium acidity, the absence of catalysis by the usual catalysts of nitrosation (halides) and the high reactivity at low acidities, are in contrast to the kinetic characteristics of other N-nitrosation reactions.This atypical behaviour is discussed in terms of possible reaction mechanisms.
- Bravo, Carlos,Herves, Pablo,Leis, J. Ramon,Pena, M. Elena
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p. 185 - 190
(2007/10/02)
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