CAS: 81-81-2; Warfarin

该化合物是一种合成抗凝胶剂,通常用于预防和治疗血栓栓塞,其作用是抑制维生素K-过氧化剂再消化酶,这是肝脏中合成维生素K依赖性凝块因素所必需的;该化合物是两种对映体(R和S)的种族混合物,其S-enantiomer作为抗凝固剂的威力要大得多;Warfarin的特点是水溶性相对较低,但有机溶剂可溶解,便于其配制各种药剂;该物质的分子分子配方为C19H16O4,分子重量约为308.34克/摩尔;其药性肿瘤学学涉及口服管理,由于现有凝固因素减少所需的时间,行动延迟开始.由于遗传多形态,饮食维生素K摄入以及与其他药物的相互作用等因素,沃法在起作用时会发生重大的个体间变化,因此必须在治疗期间仔细监测凝固参数.

结构式图片

欧盟法规

《欧盟PIC法规》统一分类与标签压力设备指令-第1组危险流体REACH注册ECHA物质欧盟农药活性物质食品接触材料-禁用CMR物质OtherC&L通报欧盟生物杀灭剂法规欧盟《生物杀灭剂法规》REACH预注册废弃物危险特性清单"欧盟管控危险化学品"ECHA物质工作场所安全标识要求化妆品禁用物质清单

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合成工艺路线路线简述

  • 合成目标产物 Warfarin 主要起始原料 4-Hydroxycoumarin And Phenethyl Alcohol And Dl-Valine
  • (文献来源)合成步骤主要原料 4-Hydroxycoumarin 和 Phenethyl Alcohol 和 Dl-Valine
2-Methoxywarfarin置于三溴化硼体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 华法林
参考文献:R和s的第一个实用的不对称合成-Warfarin
标题:R和s的第一个实用的不对称合成-Warfarin
摘要:通过使用新颖的两步"手性转换"策略和duphos-Rh(i)催化的不对称氢化反应,开发了华法林ia和ib两种对映体的高效合成方法.
DOI:10.1016/0040-4039(96)01796-0

海关参考信息

专利信息


专利号:US-2024287520-A1
优先权日:2021-06-30
标题:Method for synthesis of linkage modified oligomeric compounds
发明人:RODRIGUEZ ANDREW A
权利人:IONIS PHARMACEUTICALS INC
摘要:The present disclosure provides methods of synthesizing modified oligonucletodies and oligomeric compounds (including oligomeric compounds that are antisense agents or portions thereof) comprising a modified oligonucleotide having at least one modified internucleoside linking group. In certain embodiments, the present disclosure provides stabilized formulations of certain sulfonyl azides for use in the synthesis of olignonucleotides comprising one or more sulfonyl phosphoramidate linkages. Some embodiments provide stabilized compositions of high energy reagents that may be used in the synthesis of modified oligonucleotides, allowing for safe process scale preparation thereof.

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:WO-2004011474-A1
优先权日:2002-07-31
标题:Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-6653468-B1
优先权日:2002-07-31
标 题 :Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

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-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.
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主要参考文献


1: Atoui M, Gunda S, Lakkireddy D. Left atrial appendage closure is preferred to chronic warfarin therapy: the pro perspective. Card Electrophysiol Clin. 2015 Sep;7(3):403-13. doi: 10.1016/j.ccep.2015.05.019. Epub 2015 Jul 10. Review. doi: 10.1016/j.mgene.2015.05.003. eCollection 2015 Sep. Review.
3: Entezari-Maleki T, Dousti S, Hamishehkar H, Gholami K. A systematic review on comparing 2 common models for management of warfarin therapy; pharmacist-led service versus usual medical care. J Clin Pharmacol. 2015 Jun 22. doi: 10.1002/jcph.576. [Epub ahead of print] Review. doi: 10.1016/j.ijcard.2015.06.006. Epub 2015 Jun 15. Review. doi: 10.1542/peds.2014-2578. Review. doi: 10.3978/j.issn.2072-1439.2015.01.23. Review.
7: Watanabe H, Itoh H, Tsuchiya Y, Miyagi N, Sugiyama T, Nakai Y, Shinozaki Y, Noguchi T, Jinbu Y, Kusama M. [Reinforcement of warfarin action in a patient administered S-1]. Gan To Kagaku Ryoho. 2015 Jan;42(1):131-3. Review. Japanese. doi: 10.1146/annurev-med-051113-024633. Review. doi: 10.1161/CIRCULATIONAHA.114.010426. Review. doi: 10.1517/14740338.2015.973847. Epub 2014 Oct 24. Review. doi: 10.1016/j.tcm.2014.09.001. Epub 2014 Sep 6. Review.

合成参考文献


参考文献:10.1254/fpj.135.52
摘要:Okumura K. [Current state and perspectives of pharmacological and non-pharmacological treatment of atrial fibrillation: overview]. Nihon Yakurigaku Zasshi. 2010 Feb;135(2):52–4. doi: 10.1254/fpj.135.52.
摘要:Murayama Y, Sano I, Doi Y, Iwasaki R, Chatani T, Horiki M, Kitada M, Okuno M, Kondo S, Fukuda H, Kashihara T. [A case of type 4 gastric cancer with peritoneal dissemination complicating venous thromboembolism treated effectively by combination of S-1 and warfarin]. Gan To Kagaku Ryoho. 2010 Feb;37(2):311–4.
参考文献:10.1177/112972981001100202
摘要:Schild AF. Maintaining vascular access: the management of hemodialysis arteriovenous grafts. J Vasc Access. 2010 Apr;11(2):92–9. doi: 10.1177/112972981001100202.
参考文献:10.1002/elps.200900508
摘要:Luces CA, Warner IM. Achiral and chiral separations using MEKC, polyelectrolyte multilayer coatings, and mixed mode separation techniques with molecular micelles. Electrophoresis. 2010 Mar;31(6):1036–43.
参考文献:10.1001/archoto.2009.200
摘要:Ben Simon GJ, Cheung N, McNab AA. Delayed epistaxis in external dacryocystorhinostomy: rate and risk factors. Arch Otolaryngol Head Neck Surg. 2010 Feb;136(2):183–6. doi: 10.1001/archoto.2009.200.
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