13297-17-1Relevant articles and documents
Effective promotion of beirut reaction by-cyclodextrin in water
Sun, Tao,Zhao, Wen-Jing,Hao, Ai-You,Sun, Li-Zhen
, p. 3097 - 3105 (2011)
A mild and highly efficient, environmentally friendly procedure has been developed for the conversion from benzofurazan-N-oxides to quinoxaline di-N-oxides in the presence of-cyclodextrin in water at room temperature with excellent yields. The application of cyclodextrin precludes the use of organic solvent, and the catalyst can be recovered and reused in subsequent reactions with the same catalytic activity. Herein, the Beirut reaction is carried out in the medium of water for the first time. The reaction mechanism was proposed based on the inclusion complexation of-cyclodextrin with benzofurazan-N-oxides which was confirmed by 1H NMR, ultraviolet/visible spectrum, and infrared spectroscopy. Copyright
Synthesis, 3D-QSAR analysis and biological evaluation of quinoxaline 1,4-di-N-oxide derivatives as antituberculosis agents
Pan, Yuanhu,Li, Panpan,Xie, Shuyu,Tao, Yanfei,Chen, Dongmei,Dai, Menghong,Hao, Haihong,Huang, Lingli,Wang, Yulian,Wang, Liye,Liu, Zhenli,Yuan, Zonghui
, p. 4146 - 4153 (2016)
A series of quinoxaline 1,4-di-N-oxide derivatives variously substituted at C-2 position were synthesized and evaluated for in vitro antimycobacterial activity. Seventeen compounds exhibited potential activity (MIC ?6.25?μg/mL) against Mycobacterium tuber
Preparation method of mequindox
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Paragraph 0046-0063, (2019/02/08)
The invention provides a preparation method of mequindox. The preparation method comprises the step of performing reaction by taking ortho-nitroaniline, sodium hypochlorite and acetylacetone as raw materials, taking an NaOH/attapulgite compound as a catalyst and taking sodium carboxymethyl cellulose as a solubilizing agent and a homogenizing agent so as to obtain the mequindox. The preparation method of the mequindox, provided by the invention, realizes the purpose of one-step preparation of the mequindox, omits the intermediate treatment step of benzofurazan, and is simple in technology and high in production efficiency. The purity of the prepared mequindox product can reach 99% or more, and the total yield of the prepared mequindox product can reach 84.5% or more, which is equivalent tosingle-step yield of 90% or more, so that the prepared mequindox product has broad application prospects.
Mequindox of tritium or deuterium-labeled preparation method
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Paragraph 0052; 0055, (2017/02/09)
The invention belongs to the technical field of veterinary drug preparation, and particularly relates to a preparation method for a tritium and deuterium labeled veterinary drug mequindox. The method comprises the following steps: adopting a trace synthesis method to allow tritium gas or deuterium gas and 4-bromine-2-nitroaniline or 4-iodine-2-nitroaniline to be subjected to dehalogenation reaction under the action of a catalyst and an acid acceptor, and meanwhile, introducing tritium gas or deuterium gas alternatively to generate 4-3H-2-nitroaniline or 4-2H-2-nitroaniline; performing the oxidation reaction and the Beirut reaction to prepare the C-6 tritium labeled or deuterium labeled mequindox, wherein the obtained product is clear in labeling point, high in specific activity (12.63 Ci/mmol), high in radiochemical purity (more than 98 percent) and high in chemical purity (more than 99.5 percent). The prepared tritium labeled mequindox provides a material foundation for the research of absorption, distribution, metabolism and residue elimination rules of the mequindox in an animal body; the prepared deuterium labeled mequindox can serve as an internal standard substance for the quantitative analysis of a mequindox trace amount.