CAS: 54143-55-4; N-(Piperidin-2-Ylmethyl)-2,5-Bis(2,2,2-Trifluoroethoxy)Benzamide

该化合物是一种IC类抗心律药物,主要用于治疗某些类型的严重不规则心跳,如性纤维化和心血管心血管炎,通过阻塞心脏细胞中的钠管发挥作用,有助于稳定心膜膜,减少易感性.氟丙烯酸通常通过口服施用,以其高生物利用率为名.该物质的特点在于其水中的溶解性相对较低,可影响其体内的吸收和分布.其化学配方为C17H20F6N2O3, 其分子重量反映了其复杂的结构,其中包括一个含氟芳香环.氟丙烯酸还与潜在的副作用有关,包括动脉炎,特别是在有结构性心脏病的病人中.因此,在治疗期间必须进行仔细监测.

结构式图片

欧盟法规

REACH注册ECHA物质ECHA物质C&L通报

上下游产品

CAS号22990-77-8 2-氨甲基哌啶 | CAS号35480-31-0 2,5-双三氟乙氧基苯甲酸甲酯 | CAS号54143-56-5 醋酸氟卡胺

合成工艺路线路线简述

  • 合成目标产物 Flecainide 主要起始原料 2-Piperidylmethylamine And Methyl 2,5-Bis(2,2,2-Trifluoroethoxy)Benzoate
  • (文献来源)合成步骤主要原料 2-Piperidylmethylamine 和 Methyl 2,5-Bis(2,2,2-Trifluoroethoxy)Benzoate
N-(2-吡啶基甲基)-2,5-二(2,2,2-三氟乙氧基)苯甲酰胺 以71%的收率获得产物
参考文献:Leir,Charles M.
标题:Leir,Charles M.

海关参考信息

专利信息


专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

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-7196197-B2
优先权日:2003-09-17
标题:Process for the preparation of Flecainide, its pharmaceutically acceptable salts and important intermediates thereof
发明人:WANG ZHI-XIAN; LI YUANQIANG; GUNTOORI BHASKAR REDDY
权利人:APOTEX PHARMACHEM INC
摘要:Process for the preparation of Flecainide, its pharmaceutically acceptable salts and important intermediates thereof that involves the use of the 2-halobenzoic acid and its derivatives as a starting material. The use of this process also allows for the synthesis of a novel intermediate useful in the production of Flecainide. This new process is an inexpensive and efficient process for the manufacture of these compounds.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:WO-9964032-A1
优先权日:1998-06-08
标题 :Combinatorial synthesis of multibinding libraries
发明人:CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.

专利号:US-6599922-B2
优先权日:2001-08-10
标 题:Process for the preparation of 2,5-bis-(2,2,2-trifluoroethoxy)-N-(2-piperidylmethyl)-benzamide (FLECAINIDE)
发明人:VIGANO ENRICO; PIZZATTI ENRICA; MOLTENI RENATO; LANFRANCONI SIMONA
权利人:A M S A ANONIMA MATERIE SINT E
摘要:Process for the synthesis of FLECAINIDE comprising the reaction between 2,5-dihydroxybenzoic acid with trifluoroethanol perfluorobutanesulphonate to give the intermediate trifluoroethanol 2,5-bis-trifluoroethoxybenzoate, the reaction of said intermediate with 2-aminomethylpiperidine to give FLECAINIDE.
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主要参考文献


1: Benoit A, Paolucci M, Stefan L, Vanderperren O, Hoffer E. [A CASE OF FLECAINIDE INTOXICATION]. Rev Med Liege. 2015 Sep;70(9):442-5. Review. French. doi: 10.1007/s00228-015-1832-0. Epub 2015 Apr 15. Review.
3: Andrikopoulos GK, Pastromas S, Tzeis S. Flecainide: Current status and perspectives in arrhythmia management. World J Cardiol. 2015 Feb 26;7(2):76-85. doi: 10.4330/wjc.v7.i2.76. Review.
4: Apostolakis S, Oeff M, Tebbe U, Fabritz L, Breithardt G, Kirchhof P. Flecainide acetate for the treatment of atrial and ventricular arrhythmias. Expert Opin Pharmacother. 2013 Feb;14(3):347-57. doi: 10.1517/14656566.2013.759212. Epub 2013 Jan 7. Review. doi: 10.2165/11599950-000000000-00000. Review. doi: 10.1016/j.tcm.2012.06.008. Epub 2012 Aug 4. Review. doi: 10.1093/europace/euq517. Epub 2011 Feb 2. Review. doi: 10.1093/europace/euq382. Epub 2010 Dec 7. Review.

合成参考文献


参考文献:10.1093/europace/euq007
摘要:Guédon-Moreau L, Capucci A, Denjoy I, Morgan CC, Périer A, Leplège A, Kacet S. Impact of the control of symptomatic paroxysmal atrial fibrillation on health-related quality of life. Europace. 2010 May;12(5):634–42.
参考文献:10.1024/0369-8394.94.45.1753
摘要:Scharf C. [Atrial flutter and fibrillation]. Praxis (Bern 1994). 2005 Nov 09;94(45):1753–9. doi: 10.1024/0369-8394.94.45.1753.
参考文献:10.1007/s12471-011-0175-4
摘要:Heemstra HE, Nieuwlaat R, Meijboom M, Crijns HJ. The burden of atrial fibrillation in the Netherlands. Netherlands Heart Journal. 2011 Jul 15;19(9):373–8. doi: 10.1007/s12471-011-0175-4.
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