普拉格雷置于盐酸体系中,用 丙酮 用作溶剂,以88%的收率获得普拉格雷盐酸盐 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-12188069-B2 优先权日:2018-01-31 标 题 :Biocatalyst and methods for synthesizing mixed disulfide conjugates of thienopyridine compounds 发明人:ZHANG HAOMING 权利人:UNIV MICHIGAN REGENTS 摘要:The present invention relates to methods for synthesizing mixed disulfide conjugates of thienopyridine compounds with a genetically engineered variant of cytochrome P450 BM3 or CYP102A1 as a catalyst, and belongs to the field of chemical synthesis.
专利号:US-2022411407-A1 优先权日:2019-11-15 标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof 发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN 权利人:UNIV NORTH CAROLINA CHAPEL HILL 摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.
专利号:CN-118307511-A 优先权日:2024-04-08 标 题:Synthesis method of 2-thiopheneethanol
专利号:CN-118420476-A 优先权日:2023-02-01 标题 :A green synthesis method of procaine hydrochloride
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:10.1016/j.jacc.2011.04.017 摘要:Bonello L, Pansieri M, Mancini J, Bonello R, Maillard L, Barnay P, Rossi P, Ait-Mokhtar O, Jouve B, Collet F, Peyre JP, Wittenberg O, de Labriolle A, Camilleri E, Cheneau E, Cabassome E, Dignat-George F, Camoin-Jau L, Paganelli F. High On-Treatment Platelet Reactivity After Prasugrel Loading Dose and Cardiovascular Events After Percutaneous Coronary Intervention in Acute Coronary Syndromes. Journal of the American College of Cardiology. 2011 Jul;58(5):467–73. doi: 10.1016/j.jacc.2011.04.017.