Boc-D-Phe-Pro-Arg(Pbf)-Pro-Gly-Gly-Gly-Gly-Asn(Trt)-Gly-Asp(Tbu)-Phe-Glu(Tbu)-Glu(Tbu)-Ile-Pro-Glu(Tbu)-Glu(Tbu)-Tyr(Tbu)-Leu-Otbu置于水,三氟乙酸,十二硫醇体系中,化学反应 1.0H,以110 G的收率获得比伐卢定 参考文献:Process For Production Of Bivalirudin 标题:Process For Production Of Bivalirudin 摘要:该发明涉及制备高纯度bivalirudin的方法.该多肽以高纯度制备,至少为98.5%(通过HPLC测定),总杂质量少于1.5%,其中不超过0.5%为[asp9-Bivalirudin],每种杂质均小于1.0%,最好通过HPLC测定至少具有约99.0%的纯度,总杂质量少于1.0%,其中不超过0.5%为[asp9-Bivalirudin],每种杂质均小于0.5%.
专利号:US-7301006-B2 优先权日:2002-07-16 标 题 :Methods and materials for the synthesis of modified peptides 发明人:YOUNG TRAVIS G; KIESSLING LAURA L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove α-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified. Preferred side-chain protecting groups are chemically distinguishable from the azide-bearing protecting group and substantially orthogonal reaction conditions can be selected such that side-chain protection of other amino acids is maintained when the azide-bearing protecting group is removed. The use of the azide-bearing protecting group of this invention for one or more hydroxy amino acids during peptide synthesis allows the selective unmasking of those azide-protected side-chain hydroxyl groups and selective modification of the hydroxyl groups that are selectively unmasked. The methods and materials herein are particularly used in synthesis of sulfated, phosphorylated and glycosylated peptides and proteins. Kits and methods of synthesizing a modified peptide or protein using the kits are also provided.
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-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.
专利号:US-9388212-B2 优先权日:2013-02-21 标 题:Solid phase peptide synthesis via side chain attachment 发明人:BARLOS KLEOMENIS K 权利人:CHEMICAL & BIOPHARMACEUTICAL LAB OF PATRAS S A 摘要:The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.
参考文献:10.1007/s11239-010-0454-8 摘要:Lopes RD, Garcia D, Becker RC, Granger CB, Newby LK, Alexander JH, Jolicoeur EM, Handler A, Pieper KS, Carvalho AC, Guimaraes HP, Chamone DAF, Baruzzi AC, Machado FS, Timerman A, Lopes AC. Highlights from the II international symposium of thrombosis and anticoagulation (ISTA), October 22–23, 2009, São Paulo, Brazil. Journal of Thrombosis and Thrombolysis. 2010 Feb 16;29(4):395–408. doi: 10.1007/s11239-010-0454-8. 参考文献:10.1007/s12028-011-9591-y 摘要:Watanabe M, Siddiqui FM, Qureshi AI. Incidence and management of ischemic stroke and intracerebral hemorrhage in patients on dabigatran etexilate treatment. Neurocrit Care. 2012 Feb;16(1):203–9. doi: 10.1007/s12028-011-9591-y. 参考文献:10.2147/tcrm.s20975 摘要:Abdel-Razeq H, Ismael Y. Dealing with thrombocytopenia during anticoagulation with heparins for active venous thromboembolism: a play-it-safe practical approach. Ther Clin Risk Manag. 2011;7():213–7. 参考文献:10.1016/j.jcin.2011.04.008 摘要:Witzenbichler B, Mehran R, Guagliumi G, Dudek D, Huber K, Kornowski R, Stuckey TD, Fahy M, Parise H, Stone GW. Impact of diabetes mellitus on the safety and effectiveness of bivalirudin in patients with acute myocardial infarction undergoing primary angioplasty: analysis from the HORIZONS-AMI (Harmonizing Outcomes with RevasculariZatiON and Stents in Acute Myocardial Infarction) trial. JACC Cardiovasc Interv. 2011 Jul;4(7):760–8. doi: 10.1016/j.jcin.2011.04.008.