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4-氟苯胺置于镍 盐酸,氢气,硝酸体系中,用 乙醇 作为反应溶剂,化学反应 2.5H,反应生成 4-氟-1,2-苯二胺
参考文献:Structure-Activity Relationship Of Omeprazole And Analogs As Helicobacter Pylori Urease Inhibitors
标题:Structure-Activity Relationship Of Omeprazole And Analogs As Helicobacter Pylori Urease Inhibitors
摘要:Helicobacter Pylori Urease Belongs To A Family Of Highly Conserved Urea-Hydrolyzing Enzymes. A Common Feature Of These Enzymes Is The Presence Of Two Lewis Acid Nickel Ions And A Reactive Cysteine Residue In The Active Site. The H+/k(+)-Atpase Inhibitor Omeprazole Is A Prodrug Of A Sulfenamide Which Covalently Modifies Cysteine Residues On The Luminal Side Of The H+/k(+)-Atpase Of Gastric Parietal Cells. Omeprazole And Eight Analogues Were Selected Based On Their Chemical,Electronic,And Kinetic Properties,And Each Was Incubated With Viable H. Pylori In Phosphate-Buffered Saline At Ph 7.4 For 30 Min,After Which 100 Mm Urea Was Added And The Amount Of Ammonia Formed Analyzed After A Further 10 Min. Inhibition Between 0% And 100% At A 0.1 Mm Concentration Was Observed For The Different Analogues And Could Be Expressed As A Function Of The Pka-Value Of The Pyridine,The Pka-Value Of The Benzimidazole,The Overall Lipophilicity,And,Most Importantly,The Rate Of Sulfenamide Formation,In A Quantitative Structure-Activity Relationship. The Inhibition Was Potentiated By A Lower Ph (Favoring The Formation Of The Sulfenamide) But Abolished In The Presence Of Beta-Mercaptoethanol (A Scavenger Of The Sulfenamide). Structural Analogues Incapable Of Yielding The Sulfenamide Did Not Inhibit Ammonia Production. Treatment Of Helicobacter Felis-Infected Mice With 230 Mumol/kg Flurofamide B.I.D. For 4 Weeks,Known To Potently Inhibit Urease Activity In Vivo,As A Means Of Eradicating The Infection,Was Tested And Compared With The Effect Of 125 Mumol/kg Omeprazole B.I.D. For 4 Weeks. Neither Treatment Proved Efficacious.
DOI:10.1021/jm00025A008

专利信息

专利号:WO-2011106929-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人：MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO
权利人:MERCK SHARP & DOHME; ANGELETTI P IST RICHERCHE BIO; MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO
摘要:Compounds of formula I that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infection and for inhibiting HCV viral replication and /or viral production in a cell-based system.

专利号:US-9951049-B2
优先权日:2014-05-15
标题 :Pyrazole linked benzimidazole conjugates and a process for preparation thereof
发明人：KAMAL AHMED; SHAIK ANVER BASHA; KUMAR GAJJELA BHARATH; REDDY VANGALA SANTHOSH
权利人:COUNCIL OF SCIENT & INDUSTRIAL RESEACH; COUNCIL SCIENT IND RES
摘要:Pyrazole linked benzimidazole conjugates and a method for synthesis of one or more compounds having a pyrazole linked benzimidazole conjugate, particularly pyrazole linked benzimidazole conjugates that are useful as potential antitumor agents against human cancer cell lines, such as leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer. The process comprises the step of oxidative cyclization of o-phenylenediamines and 3-phenyl-1H-pyrazole-5-carbaldehydes with sodium metabisulphite in ethanol/methanol solvent system at a desired temperature for a period of time to obtain the pyrazole linked benzimidazole conjugate.

专利号:US-3935314-A
优先权日:1971-11-24
标题 :Anti-hypertensive compositions of benzimidazole derivatives
发明人：WATTS ERIC ALFRED
权利人:BEECHAM GROUP LTD
摘要:Antihypertensive pharmaceutical compositions comprising a compound of the formula (II) ##SPC1## n or pharmaceutically acceptable salts or solvates thereof wherein R 1 is nitrile or amidino; R 2 is hydrogen or lower hydrocarbon; R 3 , R 4 , R 5 and R 6 which may be the same or different, are each selected from hydrogen, halogen, nitro, trifluoromethyl, lower alkyl, lower acyl, hydroxyl, lower etherified hydroxyl or lower acylated hydroxyl; together with a pharmaceutically acceptable carrier. The compounds of formula (II) are also useful as intermediates in the synthesis of the corresponding 2-aminoimidazoline compounds.

专利号:US-2012328569-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人：MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN
权利人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN
摘要:Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-2013102730-A1
优先权日:2010-04-02
标 题:Polyamine-containing polymers and methods of synthesis and use
发明人：JOST ROBERT W; ULUDAG HASAN; BOLUK MEHMET YAMAN
权利人:JOST ROBERT W; ULUDAG HASAN; BOLUK MEHMET YAMAN; ALBERTA INNOVATES TECHNOLOGY FUTURES
摘要:The present invention relates to polyamine-containing polymers and methods of their synthesis and use. The polymer may be hydroxyethylcellulose, dextran, poly(vinyl alcohol) or poly(methyl acrylate).

专利号:CN-107954939-B
优先权日:2017-12-07
标 题 :A kind of method for the catalytic synthesis of benzimidazole derivatives of N,N-dimethylaminothioformyl chloride derivatives under microwave radiation