- Facile synthesis of isatins by direct oxidation of indoles and 3-iodoindoles using NIS/IBX
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A facile one-pot access to a broad range of isatins by direct oxidation of indoles using NIS/IBX reagent in DMSO at 25 °C in very good isolated yields is reported. It is shown by mechanistic investigations that a number of substituted indoles react rapidly with NIS in DMSO to produce intermediary 3-iodoindoles, which undergo oxidation subsequently to isatins with IBX.
- Chandra, Ajeet,Yadav, Navin R.,Moorthy, Jarugu Narasimha
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supporting information
p. 2169 - 2174
(2019/03/04)
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- COMPOUNDS AND METHOD OF USE
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This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.
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Paragraph 1208
(2019/09/06)
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- PhI(OAc)2/NaX-mediated halogenation providing access to valuable synthons 3-haloindole derivatives
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This paper describes a mild phenyliodine diacetate mediated method for selective chlorination, bromination, and iodination of indole C-H bonds using sodium halide as a source for analogous halogenations. The combination of NaX and phenyliodine diacetate provides an invincible system for halogenation of indoles. This protocol was compatible with a wide array of indole substrates and provides straight forward access to potential halogenated arenes.
- Himabindu, Vittam,Parvathaneni, Sai Prathima,Rao, Vaidya Jayathirtha
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p. 18889 - 18893
(2018/11/27)
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- A Versatile C–H Halogenation Strategy for Indole Derivatives under Electrochemical Catalyst- and Oxidant-Free Conditions
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Halogenated indoles are essential structural motifs in bioactive natural products. Reported herein is an economical and scalable electrochemical protocol for regioselective 3C–H halogenation of indole derivatives. This strategy provides access to a host of 3-iodo-, 3-bromo-, 3-chloro-, and 3-thiocyanoindole derivatives under mild conditions using inexpensive (pseudo)halide salts as the sole reagent. The optimized conditions do not require any supplementary electrolyte salts.
- Sun, Linhao,Zhang, Xing,Li, Zilong,Ma, Jimei,Zeng, Zhen,Jiang, Hong
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supporting information
p. 4949 - 4952
(2018/05/15)
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- Synthesis of furan-fused 1,4-dihydrocarbazoles via an unusual Garratt-Braverman Cyclization of indolyl propargyl ethers and their antifungal activity
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The reactivity of indole based bis-propargyl ethers 4a-4g under Garratt-Braverman condition (KOBut in refluxing toluene) has been studied. Interestingly, these propargyl systems with one arm attached with substituted 3-indolyl derivatives leavi
- Mandal, Arundhoti,Mandal, Santi M.,Jana, Saibal,Bag, Subhendu Sekhar,Das, Amit K.,Basak, Amit
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p. 3543 - 3556
(2018/05/25)
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- Construction of Cyclopenta[b]indol-1-ones by a Tandem Gold(I)-Catalyzed Rearrangement/Nazarov Reaction and Application to the Synthesis of Bruceolline H
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A tandem gold(I)-catalyzed rearrangement/Nazarov reaction of enynyl acetates which efficiently provides cyclopenta[b]indol-1-ones as useful precursors for the synthesis of natural and bioactive compounds is described. The synthetic potential of the method
- Scarpi, Dina,Petrovi?, Martina,Fiser, Béla,Gómez-Bengoa, Enrique,Occhiato, Ernesto G.
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supporting information
p. 3922 - 3925
(2016/08/16)
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- One-pot synthesis of camalexins and 3,3′-biindoles by the Masuda borylation-Suzuki arylation (MBSA) sequence
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The Masuda borylation/Suzuki arylation (MBSA) sequence starting from N-protected 3-iodoindoles has successfully been extended to the coupling of five-membered heterocycles and indoles in the arylation step, which could not be achieved with previously developed MBSA methods. By this approach the one-pot nature of the method as well as the use of a simple catalyst system has been retained. The applicability of the method has been demonstrated by the facile synthesis of camalexins and 3,3′-biindoles, compounds of special interest due to their pronounced antifungal, antimicrobial and cytotoxic activities. The Masuda borylation/Suzuki arylation sequence furnishes in a concise one-pot manner camalexins and 3,3′-biindoles, compounds that show pronounced antifungal, antimicrobial, and cytotoxic activities. Copyright
- Tasch, Boris O. A.,Antovic, Dragutin,Merkul, Eugen,Mueller, Thomas J. J.
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supporting information
p. 4564 - 4569
(2013/07/26)
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- Synthesis of 1-indol-3-yl-carbazoles via Garratt-Braverman cyclization
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Various indolyl carbazoles have been prepared in good yields utilizing Garratt-Braverman cyclization of bisindolyl propargyl sulfones, ethers, and amines as the key step. Georg Thieme Verlag Stuttgart · New York.
- Mukherjee, Raja,Basak, Amit
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scheme or table
p. 877 - 880
(2012/06/04)
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- One-pot synthesis of diazine-bridged bisindoles and concise synthesis of the marine alkaloid hyrtinadine A
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Diazine-bridged bisindoles are readily obtained from N-Bocprotected 3-iodoindoles and 3-iodo-7-azaindole in a pseudo three-component reaction involving a one-pot Masuda borylation-Suzuki arylation sequence. Some of the title com-pounds display promising c
- Tasch, Boris O. A.,Merkul, Eugen,Mueller, Thomas J. J.
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supporting information; experimental part
p. 4532 - 4535
(2011/10/03)
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- Automated generation and reactions of 3-hydroxymethylindoles in continuous-flow microreactors
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An automated sequential approach for the generation and reactions of 3-hydroxymethylindoles in continuous-flow microreactors is described. Consecutive halogen-magnesium exchanges of four 3-iodoindoles followed by addition to three aldehydes provided twelv
- Tricotet, Thomas,O'Shea, Donal F.
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supporting information; experimental part
p. 6678 - 6686
(2010/08/20)
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- Amino-zinc-ene-enolate cyclization: A short access to cis-3-substituted prolino-homotryptophane derivatives
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(Chemical Equation Presented) Proline chimeras are useful tools for medicinal chemistry and/or biological applications. The asymmetric synthesis of cis-3-substituted prolines can be easily achieved via amino-zinc-ene-enolate cyclization followed by transm
- Mothes, Celine,Lavielle, Solange,Karoyan, Philippe
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p. 6706 - 6710
(2008/12/22)
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- Hydroboration and Suzuki-Miyaura coupling reactions with the electronically modulated variant of an ynamine: The synthesis of (E)-β-arylenamides
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The first hydroboration of an 1-alkynylamide - the electronically modulated variant of an ynamine - is described. This hydroboration in combination with a Suzuki-Miyaura cross-coupling reaction with aryl bromides or aryl iodides allows a flexible synthesis of (E)-β-arylenamides and 3-(2'-amidovinyl)indoles with high degree of molecular diversity. (C) 2000 Elsevier Science Ltd.
- Witulski, Bernhard,Buschmann, Nicole,Bergstr??er, Uwe
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p. 8473 - 8480
(2007/10/03)
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- Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 6. 2-Indol-3-yl- and 2-azaindol-3-yl- dipyridodiazepinones
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Modification of the non-nucleoside inhibitor of HIV-1 reverse transcriptase nevirapine (Viramune) by incorporation of a 2-indolyl substituent confers activity against several mutant forms of the enzyme.
- Kelly,McNeil,Rose,David,Shih,Grob
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p. 2430 - 2433
(2007/10/03)
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