CAS: 149845-06-7; (S)-N1-((2S,3R)-4-((3S,4As,8As)-3-(Tert-Butylcarbamoyl)Octahydroisoquinolin-2(1H)-yl)-3-Hydroxy-1-Phenylbutan-2-yl)-2-(Quinoline-2-Carboxamido)Succinamide Methanesulfonate

该化合物是一种主要用于治疗艾滋病毒/艾滋病的抗逆转录病毒药物,是一种抑制艾滋病毒蛋白酶的蛋白抑制剂,对病毒复制过程至关重要;该物质似乎是白白的,白白的晶状粉,可溶于甲醇和乙醇等有机溶剂,但在水中溶解性有限;其分子配方反映了一种复杂的结构,包括多种功能组,有助于其药理活动;Sqinavir mesylate通常与其他抗逆转录病毒剂一起使用,以提高其功效,减少抗药性发展的可能性;该化合物以其较短的半衰期而著称,需要每天多剂量才能保持血液中的治疗水平;此外,它可能具有副作用,包括胃肠紊乱和与其他药物的潜在相互作用,这在治疗过程中需要仔细监测.

结构式图片

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CAS号75-75-2 甲基磺酸 | CAS号127779-20-8 沙奎那韦 | CAS号127779-20-8 沙奎那韦

合成工艺路线路线简述

    📜2-<3(S)--2(R)-Hydroxy-4-Phenylbutyl>-N-Tert-Butyldecahydro-(4As,8As)-Isoquinoline-3(S)-Carboxamide 以63的收率获得甲磺酸沙奎拉韦
    参考文献:J. Org. Chem. 1994,59,3656-3664
    标题:J. Org. Chem. 1994,59,3656-3664

    专利信息


    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-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-11845970-B2
    优先权日:2016-01-15
    标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins
    发明人:WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN
    权利人:UNIV MARYLAND
    摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.

    专利号:US-8557979-B2
    优先权日:2004-06-10
    标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
    发明人:CHOI WOO-BAEG; KOWALIK EWA
    权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
    摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

    专利号:US-6353112-B1
    优先权日:1998-07-17
    标 题:Sultams: Solid phase and other synthesis of anti-HIV compounds and compositions
    发明人:BAKER DAVID C; JIANG BIN
    权利人:UNIV TENNESSEE RES CORP
    摘要:Biologically active sultams are disclosed which have potent anti-HIV activity. A combinational method of synthesis, which uses a solid support and variants thereof, are described. Biological compositions and method of treating mammals for viral infections with compositions comprising the sultams of the invention, especially HIV are described.

    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.

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    品牌试剂参考报价(招募中)

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Muret P, Solas C; Groupe Suivi Therapeutique Pharmacologique de la Societe Francaise de Pharmacologie et de Therapeutique. [Evidence-based therapeutic drug monitoring for saquinavir]. Therapie. 2011 May-Jun;66(3):207-12. doi: 10.2515/therapie/2011029. Epub 2011 Aug 9. Review. French. doi: 10.1517/17425250903273160. Review. Review. Review. Review. Review. Review. Review. French. Review. Review. Review. Review. French. Review. Review. Review. Review. Review. Review. Review. Review.

    合成参考文献


    摘要:Gekkan Yakuji. Pharmaceuticals Monthly., 40(2183), 1998
    参考文献:10.1023/b:pham.0000008043.71001.43
    摘要:Alsenz J, Haenel E. Development of a 7-day, 96-well Caco-2 permeability assay with high-throughput direct UV compound analysis. Pharm Res. 2003 Dec;20(12):1961–9. doi: 10.1023/b:pham.0000008043.71001.43.
    参考文献:10.1023/a:1016121100568
    摘要:Hugen PWH, Burger DM, Koopmans PP, Cohen Stuart JWT, Kroon FP, van Leusen R, Hekster YA. Saquinavir soft-gel capsules (Fortovase®) give lower exposure than expected, even after a high-fat breakfast. International Journal of Clinical Pharmacy. 2002 Jun;24(3):83–6. doi: 10.1023/a:1016121100568.
    参考文献:10.1186/1758-2652-8-2-36
    摘要:Julio MS, Schutz M, Schwartz R, Jayaweera DT, Burnside AF, Walmsley S, Saag MS. Efficacy, Safety and Pharmacokinetics of Once‐Daily Saquinavir Soft‐Gelatin Capsule/Ritonavir in Antiretroviral‐Naive, HIV‐Infected Patients. Journal of the International AIDS Society. 2006 Jan;8(1):36. doi: 10.1186/1758-2652-8-2-36.
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