CAS: 174484-41-4; Tipranavir

该化合物是一种专门针对人体免疫机能丧失病毒1型(HIV-1)的无寄生虫蛋白抑制剂(PI),它通过有选择地与病毒蛋白结合,对多抗药性HIV-1菌株表现出了有力的抗药性,从而抑制了病毒成熟所必需的病毒性多蛋白的裂痕.Tipranavir具有独特的抗药性特征,因其灵活的分子结构和高抗药性而保持了抗PI的抗药性.它通常与Ritonavir共同管理,通过细胞色素P450抑制剂来增强药用基因学.临床研究表明它在治疗经验丰富的病人中有用,治疗方法有限.由于潜在的肝脏和脂类代谢作用,它的使用需要仔细监测.

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CAS号174485-72-4 5-三氟甲基吡啶-2-磺酰氯 | CAS号174485-90-6 (R)-3-((R)-1-(3... | CAS号33698-85-0 (E)-1-Chloro-2-... | CAS号174590-40-0 (4R)-3-[(3S)-3-... | CAS号188559-25-3 [R-(R*,R*)]-3-[... | CAS号188559-10-6 (4R)-3-[(2S,3S)... | CAS号188559-22-0 (2S,5R)-2-[(1S)... | CAS号188559-05-9 [R-(E)]-3-(1-Ox... | CAS号29898-25-7 1-苯基-3-己酮 | CAS号99-61-6 间硝基苯甲醛

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    📜(E)-Pent-2-Enoyl Chloride置于palladium On Activated Charcoal 吡啶,正丁基锂,2,3-二巯基丁二酸,Oxonium,Potassium Tert-Butylate,氢气,Sodium Carbonate,Copper(I) Bromide体系中,用 四氢呋喃,甲醇,二氯甲烷,乙酸乙酯 用作溶剂,化学反应 1.0H,反应生成替拉那韦
    参考文献:Asymmetric Syntheses And Absolute Stereochemistry Of 5,6-Dihydro-α-Pyrones,A New Class Of Potent Hiv Protease Inhibitors
    标题:Asymmetric Syntheses And Absolute Stereochemistry Of 5,6-Dihydro-α-Pyrones,A New Class Of Potent Hiv Protease Inhibitors
    摘要:
    Doi:10.1021/ja963434W

    海关参考信息

    专利信息


    专利号:US-7002017-B2
    优先权日:2003-03-24
    标题 :Enantioselective hydrogenation of intermediates in the synthesis of tipranavir
    发明人:KLINGLER FRANZ DIETRICH; STEIGERWALD MICHAEL; EHLENZ RICHARD
    权利人:BOEHRINGER INGELHEIM INT
    摘要:The invention relates to a process for preparing the compounds of general formula I n nby enantioselective hydrogenation of the compounds of formula II n nin the presence of special hydrogenation catalysts. The invention is characterised by high enantioselectivity, providing easy access to a category of important pharmaceutical compositions, i.e. intermediates for the synthesis of tipranavir.

    专利号:US-8987493-B2
    优先权日:2010-05-20
    标题 :Process for synthesis of silane dipeptide analogs
    发明人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN
    权利人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN; Temple University—Of the Commonwealth System of Higher Education
    摘要:The invention provides a method of preparing silane dipeptide analogs, comprising the steps of treating a solution of a substituted 1,2-oxasilolane with lithium metal to form a solution of the dilithium salt of a substituted 3-hydroxypropylsilanol, and reacting the solution of the dilithium salt of the substituted 3-hydroxypropylsilanol with a substituted enamine.

    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-2016185745-A1
    优先权日:2013-08-07
    标题:Analogs of vinaxanthone and xanthofulvin, methods of synthesis, and methods of treatments thereof
    发明人:SIEGEL DIONICIO; CHIN MATTHEW; ELIASEN ANDERS; AXELROD ABRAM
    权利人:UNIV TEXAS
    摘要:The present invention relates generally to methods of synthesis of vinaxanthone and xanthofulvin, novel analogs, and methods of use thereof.

    专利号:US-2004110957-A1
    优先权日:2002-12-05
    标 题 :Process for the synthesis of an antiviral compound
    发明人:WILKEN JOERG; NERENZ FRANK; KANSCHIK-CONRADSEN ANDREAS
    权利人:HONEYWELL INT INC
    摘要:In a process comprising synthesizing pyranes including [R—(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide the present invention comprises the improvements comprising: (a) providing a racemic mixture of 3-hydroxy-3-(2-phenylethyl)-hexanoate ethyl acetate by reacting said 1-phenyl-hexan-3-one with ethylbromoacetate under Reformatsky conditions; and (b) separating (R)-3-hydroxy-3-(2-phenylethyl)-hexanoic acid in enantiomeric excess by saponification and reverse resolution of the racemate of step (a) to produce a resolved product. In addition, the present invention comprises a reverse resolution process for separating an enantiomer from a mixture of enantiomers.

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    主要参考文献


    1: Vergani B, Rusconi S. Tipranavir in the protease inhibitors arena. Drugs R D. 2011 Dec 1;11(4):291-3. doi: 10.2165/11594570-000000000-00000. doi: 10.2165/11596340-000000000-00000. Epub 2011 Aug 17.
    6: Allavena C, Flandre P, Pugliese P, Valantin MA, Poizot-Martin I, Cabié A, Melliez H, Cuzin L, Duvivier C, Dellamonica P, Raffi F; Dat'aids Group. Tipranavir in highly antiretroviral treatment-experienced patients: Results from a French prospective cohort. Scand J Infect Dis. 2012 Jan;44(1):37-43. Epub 2011 Aug 19. Epub 2011 Aug 8.
    8: Kort JJ, Aslanyan S, Scherer J, Sabo JP, Kohlbrenner V, Robinson P. Effects of tipranavir, darunavir, and ritonavir on platelet function, coagulation, and fibrinolysis in healthy volunteers. Curr HIV Res. 2011 Jun 1;9(4):237-46. doi: 10.2174/157016211796320306. Epub 2011 May 16.

    合成参考文献


    摘要:
    摘要:US Natl Inst Health; DailyMed. Current Medication Information for APTIVUS (tipranavir) capsule, liquid filled APTIVUS (tipranavir) solution (April 2012). Available from, as of November 25, 2012:
    摘要:European Medicines Agency (EMA), The European Agency for the Evaluation of Medicinal Products, European Public Assessment Report (EPAR) for Authorized Medicinal Products for Human Use; Aptivus, Scientific Discussion p.7 (2005). Available from, as of November 26, 2012:
    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
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