- An entry to 2-(cyclobut-1-en-1-yl)-1: H -indoles through a cyclobutenylation/deprotection cascade
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A transition-metal-free strategy for the synthesis of 2-(cyclobut-1-en-1-yl)-1H-indoles under mild conditions is described herein. A series of substituted 2-(cyclobut-1-en-1-yl)-1H-indoles are accessed by a one-pot cyclobutenylation/deprotection cascade from N-Boc protected indoles. Preliminary experimental and density functional theory calculations suggest that a Boc-group transfer is involved in the underlying mechanism.
- Natho, Philipp,Yang, Zeyu,Allen, Lewis A. T.,Rey, Juliette,White, Andrew J. P.,Parsons, Philip J.
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supporting information
p. 4048 - 4053
(2021/05/19)
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- Five-membered heterocyclic oxo carboxylic acid compound and medical application thereof
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The invention relates to a five-membered heterocyclic oxo carboxylic acid compound and a medical application thereof. Specifically, the invention relates to a compound, a pharmaceutical salt, a prodrug, a hydrate, a solvate or a crystal form as shown in a formula (I), and also relates to a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the pharmaceutical composition as a secretion regulator of interferon type I, especially as an STING agonist in preparation of medicines for preventing and/or treating I-type interferon related diseases.
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Paragraph 0952; 0957-0959
(2021/05/01)
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- Cu-Catalyzed Oxidation of C2 and C3 Alkyl-Substituted Indole via Acyl Nitroso Reagents
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The selective oxidation of C2-alkyl-substituted indoles to 3-oxindole and the selective C-H oxygenation or amination of C2,C3-dialkyl-substituted indoles at C2 are reported under mild conditions. The position of the alkyl substitution on the indole directs the reaction to different pathways under similar conditions.
- Zhang, Jun,Torabi Kohlbouni, Saeedeh,Borhan, Babak
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supporting information
p. 14 - 17
(2019/01/08)
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- Structure-activity relationship (SAR) optimization of 6-(Indol-2-yl) pyridine-3-sulfonamides: Identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B
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A novel, potent, and orally bioavailable inhibitor of hepatitis C RNA replication targeting NS4B, compound 4t (PTC725), has been identified through chemical optimization of the 6-(indol-2-yl)pyridine-3-sulfonamide 2 to improve DMPK and safety properties.
- Zhang, Nanjing,Zhang, Xiaoyan,Zhu, Jin,Turpoff, Anthony,Chen, Guangming,Morrill, Christie,Huang, Song,Lennox, William,Kakarla, Ramesh,Liu, Ronggang,Li, Chunshi,Ren, Hongyu,Almstead, Neil,Venkatraman, Srikanth,Njoroge, F. George,Gu, Zhengxian,Clausen, Valerie,Graci, Jason,Jung, Stephen P.,Zheng, Yingcong,Colacino, Joseph M.,Lahser, Fred,Sheedy, Josephine,Mollin, Anna,Weetall, Marla,Nomeir, Amin,Karp, Gary M.
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p. 2121 - 2135
(2014/04/03)
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- Tandem copper-catalysed aryl and alkenyl amination reactions: The synthesis of N-functionalised indoles
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A Cu-diamine complex effectively catalyses tandem C-N bond formation on 2-(2-haloalkenyl)-aryl halide substrates, to deliver a series of N-functionalised indoles. Anilines, amides and carbamates are all effective coupling partners under the developed cond
- Hodgkinson, Roy C.,Schulz, Jurgen,Willis, Michael C.
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supporting information; experimental part
p. 432 - 434
(2009/06/28)
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- Heterocyclyl-substituted dihydroquinazolines and their use as antiviral agents
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The invention relates to heterocyclyl-substituted dihydroquinazolines of formula (I), to processes for their preparation, to medicaments containing them, and to methods for the treatment and/or prophylaxis of diseases, in particular, for use as anti-viral agents, in particular, against cytomegaloviruses.
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- HETEROCYCLYL-SUBSTITUTED DIHYDROQUINAZOLINES AND USE THEREOF AS AN ANTIVIRAL AGENT
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The invention relates to heterocyclyl-substituted dihydroquinazolines of formula (I), methods for the production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular, for use as anti-viral agents, in particular, against cytomegaloviruses.
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Page/Page column 32
(2010/02/09)
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- SYNTHESIS AND REACTIVITY OF 6-(FLUOROMETHYL)INDOLE AND 6-(DIFLUOROMETHYL)INDOLE
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The N-1 BOC protected precursors of 6-(fluoromethyl)indole and 6-(difluoromethyl)indole were prepared and deprotected via flash vacuum thermolysis.The stability of these newly prepared, unprotected indole derivatives has been characterized and compared to that of a previously known compound, 6(trifluoromethyl)indole.
- Woolridge, Elisa M.,Rokita, Steven E.
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p. 6117 - 6120
(2007/10/02)
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