4-N[2(4,6-二氯吡啶基)]-氨基苯腈置于palladium On Activated Charcoal,氢气,N,N-二异丙基乙胺体系中,用 四氢呋喃 用作溶剂,化学反应生成达匹韦林 参考文献:Optimization Of Diarylazines As Anti-Hiv Agents With Dramatically Enhanced Solubility 标题:Optimization Of Diarylazines As Anti-Hiv Agents With Dramatically Enhanced Solubility 摘要:Non-Nucleoside Inhibitors Of Hiv-1 Reverse Transcriptase Are Reported That Have Ca. 100-Fold Greater Solubility Than The Structurally Related Drugs Etravirine And Rilpivirine,While Retaining High Anti-Viral Activity. The Solubility Enhancements Come From Strategic Placement Of A Morpholinylalkoxy Substituent In The Entrance Channel Of The Nnrti Binding Site. Compound 4D Shows Low-Nanomolar Activity Similar To Etravirine Towards Wild-Type Hiv-1 And Key Viral Variants. (C) 2013 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2013.06.091
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-2007099915-A1 优先权日:2005-10-07 标题 :Inhibitors of the hiv integrase enzyme 发明人:DRESS KLAUS R; JOHNSON TED W; PLEWE MICHAEL B; TANIS STEVEN P; ZHU HUICHUN 权利人:PFIZER 摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.
专利号:US-7468375-B2 优先权日:2004-04-26 标题:Inhibitors of the HIV integrase enzyme 发明人:DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; WANG HAI; YANG ANLE; YIN CHUNFENG; ZHANG JUNHU 权利人:PFIZER 摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.
专利号:US-2009170846-A1 优先权日:2005-10-03 标题 :Inhibitors of the hiv integrase enzyme 发明人:DRESS KLAUS RUPRECHT; PLEWE MICHAEL BRUNO; JOHNSON TED WILLIAM; TANIS STEVEN PAUL; TRAN KHANH TUAN 权利人:PFIZER 摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus “HIVâ€? integrase enzyme. Formula (I).
专利号:EP-1873155-A1 优先权日:2004-04-26 标题:Inhibitors of the HIV integrase enzyme 发明人:DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; ZHU HUICHUN; ZHANG JUNHU 权利人:PFIZER 摘要:The present invention is directed to compounds of formula (I),n nand pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus ('HIV') integrase enzyme.
专利号:US-7405310-B2 优先权日:2001-03-05 标 题:Non-nucleoside reverse transcriptase inhibitors 发明人:LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA 权利人:MEDIVIR AB 摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
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合成参考文献
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