3-氟苯酚置于nitronium Tetrafluoborate体系中,用 乙腈 作为反应溶剂,化学反应 1.0H,反应生成 5-氟-2-硝基苯酚 参考文献:Non-Steroidal Dissociated Glucocorticoid Agonists: Indoles As A-Ring Mimetics And Function-Regulating Pharmacophores 标题:Non-Steroidal Dissociated Glucocorticoid Agonists: Indoles As A-Ring Mimetics And Function-Regulating Pharmacophores 摘要:We Report A Sar Of Non-Steroidal Glucocorticoid Mimetics That Utilize Indoles As A-Ring Mimetics. Detailed Sar Is Discussed With A Focus On Improving Pr And Mr Selectivity,Gr Agonism,And In Vitro Dissociation Profile. Sar Analysis Led To Compound (R)-33 Which Showed High Pr And Mr Selectivity,Potent Agonist Activity,And Reduced Transactivation Activity In The Mmtv And Aromatase Assays. The Compound Is Equipotent To Prednisolone In The Lps-Tnf Model Of Inflammation. In Mouse Cia,At 30 Mg/kg Compound (R)-33 Inhibited Disease Progression With An Efficacy Similar To The 3 Mg/kg Dose Of Prednisolone. (C) 2011 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2011.09.018
专利号:US-2016194279-A1 优先权日:2012-12-09 标 题 :One pot process for the conversion of aroyl chlorides to acyl thioureas 发明人:CHEPURI VENKATA RAMANA; BEERAN SENTHILKUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention disclose an improved one pot process for synthesis of acyl thioureas of formula (I), with yield greater than 80%, from aroyl chlorides of formula (I) wherein, R′ is an aryl or a heteroarylene group substituted with one or more groups selected from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino, carboxyl, ester, halogenated hydrocarbon or an aryl or heteroaryl; R″ and R′″ are selected independently from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino or halogenated hydrocarbon.
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专利号:RU-2077535-C1 优先权日:1991-09-18 标 题 :Derivatives of benzanilide, method of their synthesis and pharmaceutical composition exhibiting antagonism to 5-ht1 receptors
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[参考文献]: Ming-Zhi Huang, Et Al. Synthesis And Herbicidal Activity Of 2-(7-Fluoro-3-Oxo- 3,4-Dihydro-2H-Benzo[b][1,4]Oxazin-6-Yl)Isoindoline-1,3-Diones. J Agric Food Chem. 2005 Oct 5;53(20):7908-14.
合成参考文献
摘要:Baker, A.; Wirth, T., Science of Synthesis Knowledge Updates, (2017) 1, 199. 摘要:C. K. Hancock and A. D. H. Clague, J. Am. Chem. Soc. 86, 4942 (1964).