1-氨基-4-硝基萘置于sodium Hydroxide体系中,化学反应 5.0H,以89%的收率获得产物4-硝基-1-萘酚 参考文献:Antimalarial Drugs. 61. Synthesis And Antimalarial Effects Of 4-[(7-Chloro-4-Quinolinyl)Amino]-2-[(Diethylamino)Methyl]-6-Alkylphenols And Their N.Omega.-Oxides 标题:Antimalarial Drugs. 61. Synthesis And Antimalarial Effects Of 4-[(7-Chloro-4-Quinolinyl)Amino]-2-[(Diethylamino)Methyl]-6-Alkylphenols And Their N.Omega.-Oxides 摘要:A Series Of 4-[(7-Chloro-4-Quinolinyl)Amino]-2-[(Diethylamino)Methyl]-6-Alkylphenols And Their N Omega-Oxides Were Synthesized By The Condensation Of 4,7-Dichloroquinoline And 4,7-Dichloroquinoline N Omega-Oxide With Appropriately Substituted 4-Amino-2-[(Diethylamino)Methyl]-6-Alkylphenol Dihydrochlorides. The Latter Precursors Were Prepared In A Six-Step Synthesis Starting From Available 2-Alkylphenols. Several Of The Title Compounds Display Potent Antimalarial Activity In Mice. DOI:10.1021/jm00388A027
专利号:US-6894173-B2 优先权日:1999-07-09 标 题 :Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same 发明人:ZHANG LIN-HUA; ZHU LEI 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar 1 , Ar 2 , L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
专利号:US-2003166931-A1 优先权日:1999-07-09 标 题 :Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
专利号:US-2003166930-A1 优先权日:1999-07-09 标题 :Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
专利号:US-2003181718-A1 优先权日:1999-07-09 标 题 :Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
专利号:EP-1200411-B1 优先权日:1999-07-09 标题:Process for synthesis of heteroaryl-substituted urea compounds
专利号:EP-1200411-A2 优先权日:1999-07-09 标题:Novel process for synthesis of heteroaryl-substituted urea compounds
[参考文献]: Wapenaar H, Et Al. The Relevance Of Ki Calculation For Bi-Substrate Enzymes Illustrated By Kinetic Evaluation Of A Novel Lysine (K) Acetyltransferase 8 Inhibitor. Eur J Med Chem. 2017 Aug 18;136:480-486.
合成参考文献
摘要:L. K. Creamer, A. Fischer, B. R. Mann, J. Packer, R. B. Richards and J. Vaughan, J. Org. Chem. 26, 3148 (1961). 参考文献:10.1021/jm301544x 摘要:Sosič I, Mirković B, Arenz K, Stefane B, Kos J, Gobec S. Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives. J Med Chem. 2013 Jan 24;56(2):521–33. doi: 10.1021/jm301544x.