127956-24-5Relevant academic research and scientific papers
An entry to 2-(cyclobut-1-en-1-yl)-1: H -indoles through a cyclobutenylation/deprotection cascade
Natho, Philipp,Yang, Zeyu,Allen, Lewis A. T.,Rey, Juliette,White, Andrew J. P.,Parsons, Philip J.
supporting information, p. 4048 - 4053 (2021/05/19)
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.
Five-membered heterocyclic oxo carboxylic acid compound and medical application thereof
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Paragraph 0952; 0957-0959, (2021/05/01)
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.
Cu-Catalyzed Oxidation of C2 and C3 Alkyl-Substituted Indole via Acyl Nitroso Reagents
Zhang, Jun,Torabi Kohlbouni, Saeedeh,Borhan, Babak
supporting information, p. 14 - 17 (2019/01/08)
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.
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
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.
, p. 2121 - 2135 (2014/04/03)
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.
Tandem copper-catalysed aryl and alkenyl amination reactions: The synthesis of N-functionalised indoles
Hodgkinson, Roy C.,Schulz, Jurgen,Willis, Michael C.
supporting information; experimental part, p. 432 - 434 (2009/06/28)
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
Heterocyclyl-substituted dihydroquinazolines and their use as antiviral agents
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, (2008/06/13)
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.
HETEROCYCLYL-SUBSTITUTED DIHYDROQUINAZOLINES AND USE THEREOF AS AN ANTIVIRAL AGENT
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Page/Page column 32, (2010/02/09)
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.
SYNTHESIS AND REACTIVITY OF 6-(FLUOROMETHYL)INDOLE AND 6-(DIFLUOROMETHYL)INDOLE
Woolridge, Elisa M.,Rokita, Steven E.
, p. 6117 - 6120 (2007/10/02)
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.
