- ZnO-mediated regioselective C-arylsulfonylation of indoles: A facile solvent-free synthesis of 2- and 3-sulfonylindoles and preliminary evaluation of their activity against drug-resistant mutant HIV-1 reverse transcriptases (RTs)
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A ZnO-mediated one-pot solvent-free protocol for the regioselective C-arylsulfonylation of indoles is described and some novel derivatives were tested on wild type and non-nucleoside inhibitor resistant K103N and Y181C HIV-1 reverse transcriptases (RTs).
- Tocco, Graziella,Begala, Michela,Esposito, Francesca,Caboni, Pierluigi,Cannas, Valeria,Tramontano, Enzo
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- InBr3-catalyzed sulfonation of indoles: A facile synthesis of 3-sulfonyl indoles
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Indoles react smoothly with sulfonyl chlorides in the presence of a catalytic amount of indium tribromide at ambient temperature to afford the corresponding 3-arylsulfonyl indole derivatives in high yields with high regioselectivity.
- Yadav,Reddy,Krishna,Swamy
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- A simple and efficient approach for the sulfonylation of indoles catalyzed by CuI
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In this paper, a simple and efficient protocol for the chemoselective sulfonation of indoles using aryl sulfonyl chlorides in the presence of CuI is reported. The reaction proceeds under mild conditions and is applicable to indoles bearing a selection of functional groups without NH protection.
- Rahman, Matiur,Ghosh, Monoranjan,Hajra, Alakananda,Majee, Adinath
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p. 342 - 346
(2013/09/23)
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- Construction of Azacycles Based on Endo-Mode Cyclization of Allenes
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A new procedure for constructing monocyclic five- and six-membered azacycles by the endo-mode ring-closing reaction of allenylazido derivatives under neutral conditions has been developed. The azabicyclo[m.n.0] compounds were prepared by applying this newly developed procedure. The seven-membered azacycle was prepared when the allene possessing an unsubstituted carboxyl amido functionality was submitted to the basic conditions. In addition, indole and quinoline skeletons were synthesized using this procedure.
- Mukai, Chisato,Kobayashi, Minoru,Kubota, Shoko,Takahashi, Yukie,Kitagaki, Shinji
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p. 2128 - 2136
(2007/10/03)
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- 1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands
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Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which N,N-dimethyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8t and N-methyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8u showed high affinity for 5-HT6 receptors with Ki = 3.7 and 5.7 nM, respectively. Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which N,N-dimethyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8t and N-methyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8u showed high affinity for 5-HT6 receptors with Ki = 3.7 and 5.7 nM, respectively.
- Bernotas, Ronald,Lenicek, Steven,Antane, Schuyler,Zhang, Guo Ming,Smith, Deborah,Coupet, Joseph,Harrison, Boyd,Schechter, Lee E.
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p. 5499 - 5502
(2007/10/03)
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- A Facile Synthesis of 3-Sulfonyl-Substituted Indole Derivatives
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A new method for the synthesis of 3-sulfonyl-substituted indole derivatives 5 was developed starting from the easily available products of the vicarious nucleophilic substitution of hydrogen in nitroarenes 1.
- Wojciechowski, Krzysztof,Makosza, Mieczyslaw
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p. 651 - 653
(2007/10/02)
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