4,5,6,7-四氢噻吩[3,2-C]吡啶盐酸盐置于正丁基锂,Sodium Hydride,溶剂黄146,三乙胺,Sodium Hydroxide体系中,用 四氢呋喃,乙醇,正己烷,二氯甲烷,N,N-二甲基甲酰胺,Mineral Oil 用作溶剂,化学反应 24.75H,反应生成普拉格雷 参考文献:An Improvement To The Preparation Of Prasugrel Hydrochloride 标题:An Improvement To The Preparation Of Prasugrel Hydrochloride 摘要:本文介绍了一种噻吩并吡啶adp受体拮抗剂普拉格雷的高效合成方法.通过 N 保护,硼酸取代和 N 取代制备了一种噻吩吡啶中间体.以 4,5,6,7-四氢噻吩并[3,2-C]吡啶和 2-溴-1-环丙基-2-(2-氟苯基)乙-1-酮为原料,经过酸水解甲醚和随后的乙酰化反应,在七个线性步骤后得到普拉格雷,总产率为 50%. Doi:10.3184/174751913X13687269227225
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-2017077550-A1 优先权日:2015-11-02 标题 :A metal free process for the preparation of alpha-substituted carbonyl compounds from alkenes 发明人:SUDALAI ARUMUGAM; PRASAD PRAGATI KISHORE; REDDI RAMBABU 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses a novel metal free process for the regioselective synthesis of α-substituted carbonyl compounds of formula I from alkene, X is selected from the following compounds (A, B).
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.
专利号:US-10308615-B2 优先权日:2015-05-29 标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2016046560-A1 优先权日:2013-04-05 标题 :Compounds useful for the treatment of metabolic disorders and synthesis of the same
1: Nambu K, Misaki K, Uno T, Tsutsui T, Kamide T, Nakada M. Periprocedural antiplatelet medication assessed by VerifyNow for neuroendovascular treatment: Comparison of prasugrel with clopidogrel. Interv Neuroradiol. 2023 Dec 11:15910199231219019. doi: 10.1177/15910199231219019. Epub ahead of print. 18(10):e0293937. doi: 10.1371/journal.pone.0293937. Erratum for: PLoS One. 2022 Jul 28;17(7):e0272140. 4: Suyama K, Nakahara I, Matsumoto S, Morioka J, Tanabe J, Hasebe A, Watanabe S. Efficacy and Safety of Dual Antiplatelet Therapy with the Routine Use of Prasugrel for Flow Diversion of Cerebral Unruptured Aneurysms. Clin Neuroradiol. 2023 Oct 17. doi: 10.1007/s00062-023-01355-2. Epub ahead of print. 55(4):E12. doi: 10.3171/2023.7.FOCUS22654. 2023 Sep 27.
合成参考文献
参考文献:10.1007/s11239-010-0457-5 摘要:Campo G, Fileti L, Valgimigli M, Tebaldi M, Cangiano E, Cavazza C, Marchesini J, Ferrari R. Poor response to clopidogrel: current and future options for its management. Journal of Thrombosis and Thrombolysis. 2010 Feb 16;30(3):319–31. doi: 10.1007/s11239-010-0457-5. 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/s11239-010-0448-6 摘要:Schwalm JR, Ahmad M, Salehian O, Eikelboom JW, Natarajan MK. Warfarin after anterior myocardial infarction in current era of dual antiplatelet therapy: a randomized feasibility trial. Journal of Thrombosis and Thrombolysis. 2010 Feb 16;30(2):127–32. doi: 10.1007/s11239-010-0448-6. 参考文献:10.1007/s11748-011-0775-3 摘要:Sonobe M, Sato T, Chen F, Fujinaga T, Shoji T, Sakai H, Miyahara R, Bando T, Huang C, Date H. Management of patients with coronary stents in elective thoracic surgery. General Thoracic and Cardiovascular Surgery. 2011 Jul 14;59(7):477–82. doi: 10.1007/s11748-011-0775-3.