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.
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.