CAS: 188627-80-7; 2-((3R,11S,17S,20S,25As)-20-((1H-Indol-3-yl)Methyl)-3-Carbamoyl-11-(4-Guanidinobutyl)-1,9,12,15,18,21-Hexaoxodocosahydro-1H-Pyrrolo[2,1-G][1,2,5,8,11,14,17,20]Dithiahexaazacyclotricosin-17-yl)Acetic Acid

该化合物是一种合成环七甲酸酯,主要用于管理急性冠状腺综合症和腹膜冠状动脉干预,主要用来控制急性冠虫综合症,是可逆的抑制剂,是小盘上二胞胎/三胞胎受体的抑制物,防止血盘聚集和阵列形成;乙虫胺来自东南部俾格米响尾蛇的毒液,其特点是与受体的具体结合性,对激动板板块至关重要;该物质一般是静脉注射,其半衰期相对较短,需要在临床环境中持续注入;乙酰乙酸一般都具有可逆性抑制剂作用,尽管它可能与出血风险有关,特别是在有出血障碍史的病人或正在接受外科手术的病人中,其药用和药理动力学使它成为急性心血管护理的宝贵工具,有助于高危病人取得更好的结果.

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2Mpa-Har-Gly-Asp-Trp-Pro-Cys-NH2 di-isopropyl ether chlorotriisopropylsilaneeptifibatide acetate

合成工艺路线路线简述

    Mpa-Har-Gly-Asp-Trp-Pro-Cys-Nh2置于ammonium Hydroxide体系中,用 水,乙腈 用作溶剂,化学反应 2.0H,以63%的收率获得依替巴肽
    参考文献:Novel Diphenylmethyl-Derived Amide Protecting Group For Efficient Liquid-Phase Peptide Synthesis: Ajiphase
    标题:Novel Diphenylmethyl-Derived Amide Protecting Group For Efficient Liquid-Phase Peptide Synthesis: Ajiphase
    摘要:An Efficient Method For The Synthesis Of Peptides Bearing An Amide At The C-Terminal Is Described. This Method Involves The Attachment Of A C-Terminal Protecting Group Bearing Long Aliphatic Chains,Followed By The Repetition Of Simple Reaction And Precipitation Steps With The Combined Advantages Of Liquid-Phase Peptide Synthesis (Lpps) And Solid-Phase Peptide Synthesis (Spps). Using This Method,A Hydrophobic Peptide Was Successfully Synthesized In Good Yield And High Purity,Which Cannot Be Obtained Satisfactorily By Spps.
    Doi:10.1021/ol302002G

    专利信息


    专利号:US-8829157-B2
    优先权日:2004-06-14
    标 题:Process for the synthesis of cyclic heptapeptide
    发明人:SAKSENA DIVYA LAL; MURALIDHARAN CHANDRAKESAN; LOBO LESTER; PAWAR DIGAMBER SHRIPATI; MOHE NIKHIL UMESH; TARUR RADHAKISHNAN VENKATASUBRAMANIAN
    权利人:SAKSENA DIVYA LAL; MURALIDHARAN CHANDRAKESAN; LOBO LESTER; PAWAR DIGAMBER SHRIPATI; MOHE NIKHIL UMESH; TARUR RADHAKISHNAN VENKATASUBRAMANIAN; USV LTD
    摘要:The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.

    专利号:US-12351573-B2
    优先权日:2019-05-09
    标 题:Compounds for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; CHENG KAI FAN
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

    专利号:US-2023159450-A1
    优先权日:2020-05-08
    标 题 :Dimers for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; ALTITI AHMAD
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

    专利号:US-2024067694-A1
    优先权日:2021-01-04
    标 题:Synthesis of teduglutide
    发明人:GANGA RAMU VASANTHAKUMAR; PATIL NITIN; SUVARNA DEEPA SHANKAR
    权利人:BIOCON LTD
    摘要:The present invention provides for novel synthetic approach of solid phase synthesis of peptides with C-terminal Aspartic acid by anchoring the side chain carboxylic group of aspartic acid to the solid support to avoid the formation of various impurities and thus resulting in higher yield and ease the purification process. The present invention further provides the usage of free amino acids and reducing agents as antioxidants in the cleavage cocktail to negate the formation of oxidative impurities formed during the global cleavage and isolation of the peptide from solid support.

    专利号:US-7691968-B2
    优先权日:2002-05-03
    标题:Process for the synthesis of peptides amides by side-chain attachment to a solid phase
    发明人:EVANS DAVID JOHN; SIMPKIN DEAN STEVEN ANTHONY; WELLINGS DONALD ALFRED; ATHERTON ERIC
    权利人:AVECIA BIOLOG LTD
    摘要:A process is provided for the solid-phase synthesis of a peptide amide which comprises attaching an α-nitrogen protected Cα-carboxamide amino acid to a solid support by its side chain, removing the α-nitrogen protecting group, assembling a peptide chain on said α-nitrogen and then cleaving the assembled peptide amide from the solid support. Novel amino acid analogues, peptide amides and solid-phase supports are also provided.

    专利号:US-2020354404-A1
    优先权日:2019-05-09
    标 题 :Peptidomimetic agents, synthesis and uses thereof
    发明人:AL-ABED YOUSEF
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Dillinger JG, Ducrocq G, Elbez Y, Cohen M, Bode C, Pollack C Jr, Nicolau JC, Henry P, Kedev S, Wiviott SD, Sabatine MS, Mehta SR, Steg PG. Activated Clotting Time to Guide Heparin Dosing in Non-ST-Segment-Elevation Acute Coronary Syndrome Patients Undergoing Percutaneous Coronary Intervention and Treated With IIb/IIIa Inhibitors: Impact on Ischemic and Bleeding Outcomes: Insights From the TAO Trial. Circ Cardiovasc Interv. 2018 Jun;11(6):e006084. doi: 10.1161/CIRCINTERVENTIONS.118.006084. doi: 10.14740/cr675w. Epub 2018 Apr 25.
    5: Bhatia N, Sawyer RD, Ikram S. Eptifibatide-Induced Profound Thrombocytopenia After Percutaneous Intervention for Acute Coronary Syndrome: A Challenging Clinical Scenario. Methodist Debakey Cardiovasc J. 2017 Oct-Dec;13(4):248-252. doi: 10.14797/mdcj-13-4-248.
    6: Sasikumar P, AlOuda KS, Kaiser WJ, Holbrook LM, Kriek N, Unsworth AJ, Bye AP, Sage T, Ushioda R, Nagata K, Farndale RW, Gibbins JM. The chaperone protein HSP47: a platelet collagen binding protein that contributes to thrombosis and hemostasis. J Thromb Haemost. 2018 May;16(5):946-959. doi: 10.1111/jth.13998. Epub 2018 Apr 15. doi: 10.1016/j.thromres.2017.12.001. Epub 2017 Dec 5.

    合成参考文献


    参考文献:10.1155/2011/250518
    摘要:Tufano A, Cimino E, Di Minno MND, Ieranò P, Marrone E, Strazzullo A, Di Minno G, Cerbone AM. Diabetes Mellitus and Cardiovascular Prevention: The Role and the Limitations of Currently Available Antiplatelet Drugs. International Journal of Vascular Medicine. 2011;2011():1–5. doi: 10.1155/2011/250518.
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