65452-73-5Relevant academic research and scientific papers
Copper-Promoted Oxidative Intramolecular C–H Amination of Hydrazones to Synthesize 1H-Indazoles and 1H-Pyrazoles Using a Cleavable Directing Group
Zhang, Guofu,Fan, Qiankun,Zhao, Yiyong,Ding, Chengrong
supporting information, p. 5801 - 5806 (2019/08/02)
A facile and efficient synthesis of 1H-indazoles and 1H-pyrazoles through a copper-promoted oxidative intramolecular C–H amination of hydrazones using a cleavable directing group was developed. This reaction is characterized by its mild conditions, operational simplicity, readily available reagents, and excellent yields. A tentative mechanism for Cu-mediated C–H oxidative amination was proposed.
Switchable Synthesis of 3-Substituted 1H-Indazoles and 3,3-Disubstituted 3H-Indazole-3-phosphonates Tuned by Phosphoryl Groups
Chen, Guihua,Hu, Minglin,Peng, Yungui
, p. 1591 - 1597 (2018/02/10)
3-Alkyl/aryl-1H-indazoles and 3-alkyl/aryl-3H-indazole-3-phosphonates were synthesized efficiently through a 1,3-dipolar cycloaddition reaction between α-substituted α-diazomethylphosphonates and arynes under simple reaction conditions. The product distribution was controlled by the phosphoryl group, which acted both as a tuning group and a traceless group in the reaction.
Preparation method of indazole and application of indazole in medicine synthesis
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Paragraph 0067; 0080; 0081, (2017/04/21)
The invention belongs to the field of chemicals, and relates to a preparation method of indazole and an application of the indazole in medicine synthesis. The invention discloses a preparation method of indazole and an application of the indazole in synthesizing 1H-indazole-3-carboxylic acid, lonidamine, a compound 8, a compound 9, a compound 10, axitinib, YD-3, YC-1 and similar substances thereof.
Copper(I) Oxide-Mediated Cyclization of o-Haloaryl N-Tosylhydrazones: Efficient Synthesis of Indazoles
Tang, Meng,Kong, Yuanfang,Chu, Bingjie,Feng, Dan
supporting information, p. 926 - 939 (2016/04/05)
An efficient synthesis of indazoles from readily accessible E/Z mixtures of o-haloaryl N-tosylhydrazones has been developed. The thermo-induced isomerization of N-tosylhydrazones is discussed. A series of valuable indazole derivatives are prepared in good yields, and the method has been successfully applied to the synthesis of the bioactive compounds, lonidamine, AF-2785, axitinib, YC-1 and YD-3.
Elemental step thermodynamics of various analogues of indazolium alkaloids to obtaining hydride in acetonitrile
Lei, Nan-Ping,Fu, Yan-Hua,Zhu, Xiao-Qing
, p. 11472 - 11485 (2015/12/04)
A series of analogues of indazolium alkaloids were designed and synthesized. The thermodynamic driving forces of the 6 elemental steps for the analogues of indazolium alkaloids to obtain hydride in acetonitrile were determined using an isothermal titration calorimeter (ITC) and electrochemical methods, respectively. The effects of molecular structure and substituents on the thermodynamic driving forces of the 6 steps were examined. Meanwhile, the oxidation mechanism of NADH coenzyme by indazolium alkaloids was examined using the chemical mimic method. The result shows that the oxidation of NADH coenzyme by indazolium alkaloids in vivo takes place by one-step concerted hydride transfer mechanism.
ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
Youngsaye, Willmen,Hartland, Cathy L.,Morgan, Barbara J.,Ting, Amal,Nag, Partha P.,Vincent, Benjamin,Mosher, Carrie A.,Bittker, Joshua A.,Dandapani, Sivaraman,Palmer, Michelle,Whitesell, Luke,Lindquist, Susan,Schreiber, Stuart L.,Munoz, Benito
supporting information, p. 1501 - 1507 (2013/10/22)
The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substances inherently toxic to either mammalian or fungal cells. A substituted indazole possessing the desired bioactivity profile was selected for further development, and initial investigation of structure-activity relationships led to the discovery of ML212.
Synthesis of N2-(substituted benzyl)-3-(4-methylphenyl)indazoles as novel anti-angiogenic agents
Huang, Li-Jiau,Shih, Mei-Ling,Chen, Hua-Sin,Pan, Shiow-Lin,Teng, Che-Ming,Lee, Fang-Yu,Kuo, Sheng-Chu
, p. 528 - 536 (2007/10/03)
To search for novel compounds with potent anti-angiogenic activity, a series of N1-(substituted benzyl)-3-(4-methylphenyl)-1H-indazoles (16, 18, 20, 22, 24, 26, 28, 30, 32) and N2-(substituted benzyl)-3-(4-methylphenyl)-2H-indazoles
Synthesis of N2 - (substituted arylmethyl) -3- (substituted phenyl) indazoles as novel anti-angiogenic agents
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Page/Page column 4, (2008/06/13)
Novel compounds of 2-(substituted arylmethyl)-3-(substituted phenyl)-2H-indazoles and 1-(substituted arylmethyl)-3-(substituted phenyl)-1H-indazoles are synthesized, and useful as anti-angiogenic agents.
