CAS: 269055-15-4; 4-((6-Amino-5-Bromo-2-((4-Cyanophenyl)Amino)Pyrimidin-4-yl)Oxy)-3,5-Dimethylbenzonitrile

该化合物是非核反转转转录酶抑制剂,主要用于治疗艾滋病毒-1感染,其特点是能够抑制反转发发发酶酶,这对病毒的复制至关重要,乙酸乙酰因广泛防治各种艾滋病毒菌株而闻名,包括抗其他NRTI的菌株,使其成为抗逆转录病毒疗法的宝贵选择,该化合物具有复杂的化学结构,有助于其独特的药理特性,通常通过口服,并经常与其他抗逆转病毒剂结合使用,以提高效力和降低抗药性发展的风险,乙酰胺主要通过肝脏代谢,涉及细胞色素P450酶,可导致与其他药物的药物相互作用,常见副作用包括皮疹,恶心和疲劳,但一般都很好地表现出来.总体而言,乙型乙型六氯环己烷是艾滋病毒治疗的一个重要进步,特别是对治疗经验感染的病人而言.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

4-[[5-bromo-4-(4-cyano-2,6-dimethylphenoxy)-6-chloro-2-pyrimidinyl]amino]-benzonitrile 4-(4,6-dichloropyrimidine-2-yl-amino)benzonitrile 4-((4,6-dihydroxypyrimidine-2-yl)amino)benzonitrile 4-[[(5-bromo-4,6-dichloro)-2-pyrimidinyl]amino]benzonitrile 4-[[4-amino-5-bromo-6-(4-cyano-2,6-dimethylphenyloxy)-2-pyrimidinyl]amino]benzonitrile hydrobromide etravirine tosylatee salt etravirine phosphate etravirine hydr°Chloride salt

合成工艺路线路线简述

  • 合成目标产物 Etravirine 主要起始原料 6-Desamino 6-Chloro Etravirine
  • (文献来源)合成步骤主要原料 6-Desamino 6-Chloro Etravirine
4-[[4-Amino-5-Bromo-6-(4-Cyano-2,6-Dimethylphenyloxy)-2-Pyrimidinyl]Amino]Benzonitrile Hydrobromide置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应 1.25H,反应生成依曲韦林
参考文献: Polymorphs Of Etravirine And Processes For Preparation Thereof[fr] Formes Polymorphes D'étravirine Et Leurs Procédés De Préparation
标题: Polymorphs Of Etravirine And Processes For Preparation Thereof[fr] Formes Polymorphes D'étravirine Et Leurs Procédés De Préparation

海关参考信息

专利信息


专利号:US-2015336900-A1
优先权日:2012-10-29
标题 :Process for the Synthesis of Etravirine and Its Intermediates
发明人:PULLAGURLA MANIK REDDY; RANGISETTY JAGADEESH BABU; NANDAKUMAR MECHERIL VALSAN
权利人:BIOPHORE INDIA PHARMACEUTICALS PVT LTD
摘要:The invention discloses the synthesis of Etravirine via intermediate 4-((4-amino-5-bromo-6-chloropyrimidin-2-yl) amino)benzonitrile and process for the preparation of Etravirine of the formula-I.

专利号:US-2010261876-A1
优先权日:2007-09-25
标 题:Novel methods of synthesis for therapeutic antiviral peptides
发明人:BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E
权利人:BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E
摘要:Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

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-2025179033-A1
优先权日:2021-12-30
标 题 :New antiviral triazole derivatives, their synthesis and their use for treatment of mammalian viral infections
发明人:MAKAROV VADIM; RIABOVA OLGA; LANE THOMAS R; EKINS SEAN
权利人:COLLABORATIONS PHARMACEUTICALS INC; FEDERAL RES CENTER FUNDAMENTALS OF BIOTECHNOLOGY RUSSIAN ACADEMY OF SCIENCE
摘要:A family of triazole derivatives is described. Also described is the use of these triazole derivatives in treating or preventing viral infections, such as human immunodeficiency virus (HIV) infections, and the diseases caused by these infections, such as acquired immunodeficiency syndrome (AIDS). The triazole derivatives, for example, comprise a central triazole group with two substituents comprising an aryl or heteroaryl group. Exemplary derivatives showed excellent HIV inhibitory activity against both wild-type and selected mutant strains of HIV.

专利号:US-9084758-B2
优先权日:2012-07-24
标题:Antiviral compositions comprising ethanol extract of Tetracera scandens and use thereof
发明人:YOU JI CHANG
权利人:CATHOLIC UNIV KOREA INDUSTRY ACADEMIC COOPERATION FOUNDATION
摘要:A composition for preventing or treating a viral infection, which includes an ethanol extract of Tetracera scandens as an effective component, is provided. The composition exhibits low toxicity and few side effects and effectively inhibits reverse transcriptase activities to suppress synthesis of DNA, and thus can be useful in preventing or treating infections caused by various kinds of RNA viruses.
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主要参考文献


1: Nelson M, Hill A, van Delft Y, Moecklinghoff C. Etravirine as a Switching Option for Patients with HIV RNA Suppression: A Review of Recent Trials. AIDS Res Treat. 2014;2014:636584. doi: 10.1155/2014/636584. Epub 2014 Feb 25. Review.
2: Casado JL. Liver toxicity in HIV-infected patients receiving novel second-generation nonnucleoside reverse transcriptase inhibitors etravirine and rilpivirine. AIDS Rev. 2013 Jul-Sep;15(3):139-45. Review. doi: 10.1517/14656566.2013.787411. Epub 2013 Apr 8. Review. doi: 10.1007/s40265-013-0022-6. Review. doi: 10.2165/11209110-000000000-00000. Review. doi: 10.2165/11534740-000000000-00000. Review. doi: 10.1517/17425255.2010.535811. Review. doi: 10.1586/erp.10.55. Review. Review. doi: 10.3851/IMP1652. Review. doi: 10.3851/IMP1651. Review. doi: 10.1089/aid.2009.0293. Review. Review. doi: 10.1016/S0213-005X(09)73219-7. Review. Spanish. doi: 10.1016/S0213-005X(09)73218-5. Review. Spanish. doi: 10.1016/S0213-005X(09)73217-3. Review. Spanish. doi: 10.1016/S0213-005X(09)73216-1. Review. Spanish. doi: 10.1016/S0213-005X(09)73215-X. Review. Spanish. doi: 10.1016/S0213-005X(09)73214-8. Review. Spanish. doi: 10.1016/S0213-005X(09)73213-6. Review. Spanish.

合成参考文献


参考文献:10.1097/qad.0b013e3283372d76
摘要:Nozza S, Galli L, Visco F, Soria A, Canducci F, Salpietro S, Gianotti N, Bigoloni A, Torre LD, Tambussi G, Lazzarin A, Castagna A. Raltegravir, maraviroc, etravirine: an effective protease inhibitor and nucleoside reverse transcriptase inhibitor-sparing regimen for salvage therapy in HIV-infected patients with triple-class experience. AIDS. 2010 Mar 27;24(6):924–8. doi: 10.1097/qad.0b013e3283372d76.
参考文献:10.1086/650732
摘要:Llibre JM, Schapiro JM, Clotet B. Clinical implications of genotypic resistance to the newer antiretroviral drugs in HIV-1-infected patients with virological failure. Clin Infect Dis. 2010 Mar 15;50(6):872–81. doi: 10.1086/650732.
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