613679-11-1Relevant academic research and scientific papers
A general and scalable synthesis of polysubstituted indoles
Diana-Rivero, Raquel,García-Tellado, Fernando,Tejedor, David
, (2021/06/14)
A consecutive 2-step synthesis of N-unprotected polysubstituted indoles bearing an electron-withdrawing group at the C-3 position from readily available nitroarenes is reported. The protocol is based on the [3,3]-sigmatropic rearrangement of N-oxyenamines generated by the DABCO-catalyzed reaction of N-arylhydroxylamines and conjugated terminal alkynes, and delivers indoles endowed with a wide array of substitution patterns and topologies.
Decarboxylative acylation of: N -free indoles enabled by a catalytic amount of copper catalyst and liquid-assisted grinding
Yu, Jingbo,Zhang, Chao,Yang, Xinjie,Su, Weike
supporting information, p. 4446 - 4451 (2019/05/16)
A facile decarboxylative acylation of N-free indoles with α-ketonates via liquid-assisted grinding was reported. The reaction requires only a catalytic amount of Cu(OAc)2·H2O in combination with O2 as the terminal oxidant to give various 3-acylindoles with high efficiency. Additionally, this new methodology was applicable to a gram-scale synthesis.
Synthesis of 3-acylindoles by oxidative rearrangement of 2-aminochalcones using a hypervalent iodine reagent and cyclization sequence
Nakamura, Akira,Tanaka, Satoshi,Imamiya, Akira,Takane, Reo,Ohta, Chiaki,Fujimura, Kazuma,Maegawa, Tomohiro,Miki, Yasuyoshi
supporting information, p. 6702 - 6705 (2017/08/22)
An efficient one-pot method was developed for the construction of 3-acylindoles via oxidative rearrangement of 2-aminochalcones followed by intramolecular cyclization. The reaction was used to convert a variety of 2-aminochalcones into 3-acylindoles in mo
Palladium catalyzed addition of arylboronic acid or indole to nitriles: Synthesis of aryl ketones
Das, Tuluma,Chakraborty, Amarnath,Sarkar, Amitabha
supporting information, p. 7198 - 7202 (2015/01/09)
Aryl ketones can be synthesized conveniently by a palladium catalyzed addition of arylboronic acid to nitriles in aqueous triflic acid. This catalytic system was extended to the addition of unprotected indoles to nitriles under a slightly modified condition to produce 3-acyl indoles in good yields.
S1P RECEPTORS MODULATORS
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Page/Page column 63, (2010/04/30)
The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
Synthesis and biological evaluation of (3,4,5-trimethoxyphenyl)indol-3-ylmethane derivatives as potential antivascular agents
Dupeyre, Gregory,Chabot, Guy G.,Thoret, Sylviane,Cachet, Xavier,Seguin, Johanne,Guenard, Daniel,Tillequin, Francois,Scherman, Daniel,Koch, Michel,Michel, Sylvie
, p. 4410 - 4426 (2007/10/03)
Combretastatin A-4 (CSA-4), a stilbene derivative, is a potent vascular disrupting agent (VDA) with the structural requirement of a cis-configuration to maintain a molecular geometry and a correct orientation of both phenyl groups. A series of indolic ana
Indole compounds as inhibitors of tubulin polymerisation for the treatment of angiogenesis-related disorders
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Page/Page column 11, (2010/02/10)
Indole compounds of the formula: wherein L1 is CO; L2 is a bond; R1 is aryl or heteroaryl; R2 is H, aryl, heteroaryl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO2
Indole compounds
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, (2008/06/13)
This invention relates to methods of inhibiting tubulin polymerization and treating cancer and other angiogenesis-related disorders with indole compounds of the formula: wherein L1, L2, R1, R2, Ra, R
Indole compounds
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, (2008/06/13)
Indole compounds of the formula: wherein L1, L2, R1, R2, Ra, Rb, Rc, Rd, and Re are defined herein. Also disclosed are methods of using of the indole compou
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents
Liou, Jing-Ping,Chang, Yi-Ling,Kuo, Fu-Ming,Chang, Chun-Wei,Tseng, Huan-Yi,Wang, Chiung-Chiu,Yang, Yung-Ning,Chang, Jang-Yang,Lee, Shiow-Ju,Hsieh, Hsing-Pang
, p. 4247 - 4257 (2007/10/03)
The synthesis and study of the structure-activity relationships of two new classes of synthetic antitubulin compounds based on 1-aroylindole and 3-aroylindole skeletons are described. Lead compounds 3, 10, and 14 displayed potent cytotoxicities with ICsu
