5-溴-2-硝基苯胺置于四(三苯基膦)钯,Palladium On Activated Charcoal,甲酸铵,Potassium Carbonate体系中,化学反应生成4-甲氧基邻苯二胺 参考文献:Identification Of Novel Hdac Inhibitors Through Cell Based Screening And Their Evaluation As Potential Anticancer Agents 标题:Identification Of Novel Hdac Inhibitors Through Cell Based Screening And Their Evaluation As Potential Anticancer Agents 摘要:A Series Of Benzimidazole Based Hdac Inhibitors Have Been Rationally Designed,Synthesized And Screened. The Sar Of This New Chemotype Is Described. The Lead Compound,11E,Showed Strong Activity In Several Cellular Assays And Demonstrated In Vivo Efficacy In Mouse Xenograft Pancreatic Cancer Models. (C) 2013 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2013.07.001
专利信息
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-9440991-B2 优先权日:2013-12-23 标 题:Synthesis of an antiviral compound 发明人:CAGULADA AMY; CHAN JOHANN; CHAN LINA; COLBY DENISE A; KARKI KAPIL KUMAR; KATO DARRYL; KEATON KATIE ANN; KONDAPALLY SUDHA; LEVINS CHRIS; LITTKE ADAM; MARTINEZ RUBEN; PCION DOMINIKA; REYNOLDS TROY; ROSS BRUCE; SANGI MICHAEL; SCHRIER ADAM J; SENG PAMELA; SIEGEL DUSTIN; SHAPIRO NATHAN; TANG DONALD; TAYLOR JAMES G; TRIPP JONATHAN; WALTMAN ANDREW W; YU LAWRENCE 权利人:GILEAD SCIENCES INC 摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
专利号:US-7501526-B2 优先权日:2005-01-20 标题 :Synthesis of polyamine compounds 发明人:WU CHIEN-HUANG; ZHU JIA-LIANG; TSENG CHEN-TSO; YEN CHI-FENG; SHIA KAK-SHAN; XIANG YIBIN; HAKIMELAHI GHOLAM HOSSEIN; CHOU MING-CHEN 权利人:TAIGEN BIOTECHNOLOGY CO LTD 摘要:This invention relates to methods of preparing the compounds of formula (V): n nEach variable in this formula is defined in the specification.
专利号:WO-2004092142-A1 优先权日:2003-04-17 标 题:An improved process for manufacture of substituted benzimidazoles 发明人:VYAS KETAN DHANSUKHAL; SINGH DHARMENDRA; NANDAVADEKAR SANJAY; BHISE SANJAY; JADHAV ATUL; DESAI HEMAL 权利人:IPCA LAB LTD; VYAS KETAN DHANSUKHAL; SINGH DHARMENDRA; NANDAVADEKAR SANJAY; BHISE SANJAY; JADHAV ATUL; DESAI HEMAL 摘要:The present invention relates to a process for the production of benzimidazole derivatives comprising providing an amino acetamido benzene derivative; and condensing and cyclising the aminoacetamido benzene derivative in the presence of a base and in the presence of a cyclising agent under conditions effective to form the benzimidazole derivative. The acetamido benzene derivative has the formula (I) wherein R is OMe or OCHF2. The resulting substituted benzimidazoles are key intermediates in the synthesis of H<+>/K<+>-ATPase irreversible inhibitors, most particularly Omeprazole.
专利号:US-2017210756-A1 优先权日:2013-12-23 标题 :Synthesis of an antiviral compound
专利号:CN-113121446-B 优先权日:2021-05-14 标题 :A kind of method for continuous flow synthesis of 2-mercapto-5-methoxybenzimidazole
摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 14. 摘要:Tymoshenko, D. O., Science of Synthesis Knowledge Updates, (2012) 3, 348. 摘要:Zhang, J., Science of Synthesis Knowledge Updates, (2013) 2, 237. 摘要:P.Vetesnik, J. Bielavsky, J. Kavalek and M. Vecera. Coll. Czech. Chem. Comm. 33, 2902 (1968).