59016-93-2 + 73096-42-1 + 138402-05-8 = 138402-11-6 反应条件:1.1 Catalysts: Zinc Triflate Solvents: Acetonitrile; 24 H,Reflux1.2 Reagents: Sodium Carbonate Catalysts: [1,1′-Bis(Diphenylphosphino)Ferrocene]Dichloropalladium Solvents: 1,2-Dimethoxyethane,Water; 24 H,Reflux1.3 Reagents: Dibromotriphenylphosphorane,Diisopropylethylamine Solvents: Dichloromethane; 18 H,Rt1.4 Reagents: Sodium Hydride Solvents: Dimethylformamide; 1 H,40 °C1.5 Catalysts: Tetrabutylammonium Iodide; 20 H,45 °C1.6 Solvents: Dichloromethane; Rt 标题:Original Loading And Suzuki Conditions For The Solid-Phase Synthesis Of Biphenyltetrazoles. Application To The First Solid-Phase Synthesis Of Irbesartan 作者:Cousaert,Nicolas; Willand,Nicolas; Gesquiere,Jean-Claude; Tartar,Andre; Deprez,Benoit; Et Al 参考文献:Tetrahedron Letters 日期:2008 卷标:49(17) 页码:2743-2747
3-[2'-(1H-Tetrazol-5-yl)-Biphenyl-4-Ylmethyl]-2-Thiophen-2-Yl-1,3-Diaza-Spiro[4.4]Non-1-En-4-One置于raney Nickel 氢气体系中,用 甲醇 用作溶剂,以84%的收率获得厄贝沙坦 参考文献: Process For The Preparation Of Irbesartan And Intermediate Products[fr] Processus Destiné à La Préparation D'Irbésartan Et De Produits Intermédiaires 标题: Process For The Preparation Of Irbesartan And Intermediate Products[fr] Processus Destiné à La Préparation D'Irbésartan Et De Produits Intermédiaires 摘要:本发明涉及一种生产厄贝沙坦的新方法,该药物化学名称为2-正丁基-4-螺环戊烷-1-[(2'-(噁唑唑-5-基)联苯-4-基)甲基]-2-咪唑啉-5-酮及其药理学上可接受的盐.此外,该发明涉及适用于生产厄贝沙坦的新(中间)化合物.
专利号:US-2008103312-A1 优先权日:2006-08-29 标 题:Processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole 发明人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D 权利人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D 摘要:Provided are processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole, an intermediate useful in the synthesis of irbesartan.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-2008214637-A1 优先权日:2004-11-11 标题 :Process for the Synthesis of Tetrazoles 发明人:ANTONCIC LJUBOMIR; LUDESCHER JOHANNES 权利人:LEK PHARMACEUTICALS 摘要:A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-6271375-B1 优先权日:1997-06-30 标 题 :Ortho-metalation process for the synthesis of 2-substituted-1-(tetrazol-5-yl)benzenes 发明人:VILLA MARCO; ALLEGRINI PIETRO; ARRIGHI KATIUSCIA; PAIOCCHI MAURIZIO 权利人:ZAMBON SPA 摘要:A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.
1: Zhang F, Zhou G, Guo L, Lu F, Zhou G. Comparison of clinical efficacy of metoprolol combined with irbesartan and hydrochlorothiazide and non-invasive ventilator in the emergency treatment of patients with severe heart failure. Exp Ther Med. 2018 Dec;16(6):5059-5066. doi: 10.3892/etm.2018.6828. Epub 2018 Oct 4. 2: Ashour S, Bayram R. Selective and validated kinetic spectrophotometric method for the determination of irbesartan in pure and pharmaceutical formulations. Ann Pharm Fr. 2018 Nov 21. pii: S0003-4509(18)30114-7. doi: 10.1016/j.pharma.2018.09.002. [Epub ahead of print] doi: 10.1002/cmdc.201800638. Epub 2018 Nov 15. doi: 10.3892/etm.2018.6669. Epub 2018 Aug 30. 5: Boccellino M, Di Domenico M, Donniacuo M, Bitti G, Gritti G, Ambrosio P, Quagliuolo L, Rinaldi B. AT1-receptor blockade: Protective effects of irbesartan in cardiomyocytes under hypoxic stress. PLoS One. 2018 Oct 24;13(10):e0202297. doi: 10.1371/journal.pone.0202297. eCollection 2018.
合成参考文献
参考文献:10.1254/fpj.135.59 摘要:Kumagai K. [Upstream approach for atrial fibrillation]. Nihon Yakurigaku Zasshi. 2010 Feb;135(2):59–61. doi: 10.1254/fpj.135.59. 参考文献:10.1007/s11596-010-0109-1 摘要:Zhao G, Zhao H, Tu L, Xu X, Zheng C, Jiang M, Wang P, Wang D. Effects and mechanism of irbesartan on tubulointerstitial fibrosis in 5/6 nephrectomized rats. J Huazhong Univ Sci Technolog Med Sci. 2010 Feb;30(1):48–54. doi: 10.1007/s11596-010-0109-1. 参考文献:10.1684/epd.2010.0293 摘要:Lapenta L, Di Bonaventura C, Fattouch J, Bonini F, Petrucci S, Gagliardi S, Casciato S, Manfredi M, Prencipe M, Giallonardo AT. Focal epileptic seizure induced by transient hypoglycaemia in insulin-treated diabetes. Epileptic Disord. 2010 Mar;12(1):84–7. doi: 10.1684/epd.2010.0293. 参考文献:10.4061/2011/132405 摘要:Tedla FM, Brar A, Browne R, Brown C. Hypertension in Chronic Kidney Disease: Navigating the Evidence. International Journal of Hypertension. 2011;2011():1–9. doi: 10.4061/2011/132405. 参考文献:10.4061/2011/516237 摘要:Rabkin SW. Endothelin but Not Angiotensin II May Mediate Hypertension-Induced Coronary Vascular Calcification in Chronic Kidney Disease. International Journal of Nephrology. 2011;2011():1–7. doi: 10.4061/2011/516237.