- Preparation method of 2,6-dibromoaniline
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The invention discloses a preparation method of 2,6-dibromoaniline. According to the method, 2,6-difluorobenzonitrile is used as an initial raw material, and the 2,6-dibromoaniline is synthesized through six steps of reactions including ammonolysis, diazotization bromination, re-ammonolysis, re-diazotization bromination, amidation and Hofmann degradation. The 2,6-dibromoaniline obtained in the process is a brown solid, and the purity of the 2,6-dibromoaniline is 98% or above.
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Paragraph 0018; 0021; 0026; 0029
(2020/08/27)
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- Site-Selective Copper-Catalyzed Amination and Azidation of Arenes and Heteroarenes via Deprotonative Zincation
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Arene amination is achieved by site-selective C-H zincation followed by copper-catalyzed coupling with O-benzoylhydroxylamines under mild conditions. Key to this success is ortho-zincation mediated by lithium amidodiethylzincate base that is effective for a wide range of arenes, including nonactivated arenes bearing simple functionalities such as fluoride, chloride, ester, amide, ether, nitrile, and trifluoromethyl groups as well as heteroarenes including indole, thiophene, pyridine, and isoquinoline. An analogous C-H azidation is also accomplished using azidoiodinane for direct introduction of a useful azide group onto a broad scope of arenes and heteroarenes. These new transformations offer rapid access to valuable and diverse chemical space of aminoarenes. Their broad applications in organic synthesis and drug discovery are demonstrated in the synthesis of novel analogues of natural product (-)-nicotine and antidepressant sertraline by late-stage amination and azidation reactions.
- Hendrick, Charles E.,Bitting, Katie J.,Cho, Seoyoung,Wang, Qiu
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p. 11622 - 11628
(2017/08/30)
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- TETRAZOLE COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Described herein are tetrazole compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tetrazole compounds are provided. The compounds are contemplated to have activity against meth
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Page/Page column 58
(2012/08/08)
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- CHEMICAL COMPOUNDS
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A compound of the formula (I) where W is N, NO, or C-R3; X is N, NO or C-R4; Y is N, NO, or C-R5; A is, for example, NR1R6; R1 and R6, independently of each other, are selected,
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Page/Page column 80
(2009/09/04)
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- Antifolate and Antibacterial Activities of 5-Substituted 2,4-Diaminoquinazolines
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A series of 5-substituted 2,4-diaminoquinazolines (3) has been synthesized and evaluated as inhibitors of the enzyme dihydrofolate reductase (DHFR) from both bacterial and mammalian sources.The best compounds (e.g. 53) show good activity against Escherichia coli DHFR, but there is no significant selectivity for the bacterial over the mammalian enzyme.The structure-activity relationships for enzyme inhibition appear to be complex and not amenable to simple analysis; a hypotesis to explain the observed qualitative structure-activity relationships is proposed.The inhibitory activities of the compounds against the growth of intact bacterial cells in vitro closely parallel those for the inhibition of the isolated bacterial enzymes, suggesting that their antifolate action is responsible for their antibacterial effects.Five of the compounds were tested for their ability to cure a systemic E. coli infection in the mouse, but they showed no therapeutic effects at their maximum tolerated doses.
- Harris, Neil V.,Smith, Christopher,Bowden, Keith
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p. 434 - 444
(2007/10/02)
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- N-(Aminophenyl)oxamic Acids and Esters as Potent, Orally Active Antiallergy Agents
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A series of N-(2-cyano-substituted-phenyl)oxamates was prepared by acylation of the appropriate anthranilonitrile with ethyloxalyl chloride.Hydrolysis with sodium hydroxide gave the corresponding oxamic acid sodium salts.These compounds were extremely potent when tested in the rat passive cutaneous anaphylaxis (PCA assay either by the ip or the po route of administration).One of the sodium salts, oxoacetic acid sodium salt (11a, Wy-41 195), has ED50 value of 0.07 mg/kg po and has been selected for further evaluation.
- Klaubert, Dieter H.,Sellstedt, John H.,Guinosso, Charles J.,Capetola, Robert J.,Bell, Stanley C.
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p. 742 - 748
(2007/10/02)
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