4-苄氧基-1-硝基苯置于盐酸,Sodium Sulfide,Ammonium Hydroxide,Palladium 10% On Activated Carbon,氢气,Potassium Carbonate,三乙胺,Potassium Iodide,Sodium Hydroxide,Sodium Nitrite体系中,用 甲醇,乙醇,水,溶剂黄146,乙酸乙酯,丙酮 作为反应溶剂,-5.0~80.0 °C,700.01 Kpa 条件下,反应 2.0H,反应生成 阿哌沙班 参考文献: Process For The Preparation And Purification Of Apixaban[fr] Procédé De Préparation Et De Purification D'Apixaban 标题: Process For The Preparation And Purification Of Apixaban[fr] Procédé De Préparation Et De Purification D'Apixaban 摘要:本发明提供了一种阿匹沙班的制备和纯化过程.
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:WO-2014072884-A1 优先权日:2012-11-12 标 题 :Process for the synthesis of apixaban 发明人:JAYARAMAN VENKAT RAMAN; PATEL NILAV; BORSANIYA MANOJ; KANZARIYA KAMLESH; RANA PIYUSH; SHAH SUDHIR; PANCHASARA DINESH; TOMER SANJIV 权利人:ALEMBIC PHARMACEUTICALS LTD; JAYARAMAN VENKAT RAMAN 摘要:The present invention relates to the Process for the preparation of Apixaban and novel intermediates useful in the synthesis of Apixaban (I).
专利号:US-7153960-B2 优先权日:2001-12-10 标 题:Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones 发明人:ZHOU JIACHENG; OH LYNETTE M; MA PHILIP; LI HUI-YIN; CONFALONE PASQUALE 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. n nThese compounds are useful as factor Xa inhibitors.
专利号:US-9920051-B2 优先权日:2014-10-15 标题:Key intermediates and impurities of the synthesis of apixaban: apixaban glycol esters 发明人:BRASOLA ELENA; TOMASI FILIPPO 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an improved process for the preparation of Apixaban, through new intermediates which undergo to a faster amidation reaction. Impurities of Apixaban are also identified and quantified.
专利号:US-2018370905-A1 优先权日:2013-04-05 标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
1: Touma L, Filion KB, Atallah R, Eberg M, Eisenberg MJ. A meta-analysis of randomized controlled trials of the risk of bleeding with apixaban versus vitamin K antagonists. Am J Cardiol. 2015 Feb 15;115(4):533-41. doi: 10.1016/j.amjcard.2014.11.039. Epub 2014 Dec 2. Review. doi: 10.2147/DDDT.S51006. eCollection 2014. Review. 3: Hanna MS, Mohan P, Knabb R, Gupta E, Frost C, Lawrence JH. Development of apixaban: a novel anticoagulant for prevention of stroke in patients with atrial fibrillation. Ann N Y Acad Sci. 2014 Nov;1329:93-106. doi: 10.1111/nyas.12567. Epub 2014 Nov 5. Review. 4: Moorman ML, Nash JE, Stabi KL. Emergency surgery and trauma in patients treated with the new oral anticoagulants: dabigatran, rivaroxaban, and apixaban. J Trauma Acute Care Surg. 2014 Sep;77(3):486-94; quiz 486-94. doi: 10.1097/TA.0000000000000360. Review. Review. doi: 10.1016/j.ejvs.2014.05.001. Epub 2014 Jun 18. Review. Review. doi: 10.1016/j.jmv.2014.02.001. Epub 2014 Mar 18. Review. French. doi: 10.4103/0976-500X.124409. Review.
合成参考文献
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