CAS: 1951-25-3; (2-Butylbenzofuran-3-yl)(4-(2-(Diethylamino)Ethoxy)-3,5-Diiodophenyl)Methanone

该化合物是一种复杂的有机化合物,主要用作治疗各种类型心律紊乱的抗体药物,其化学配方为C25H29I2N,表明含有碳,氢,碘和氮原子.阿米奥达龙的特点是其脂体性质,允许其累积于各种组织,特别是肺部,肝脏和甲状腺.该物质具有很长的半衰期,即使停止治疗后也会导致长期影响.它的作用是抑制肾刺激,延长心肌行动潜力,影响离子渠道,有助于稳定心脏的节奏.阿米奥达龙也因其潜在的副作用而闻名,包括甲状腺功能失调,肺毒性和皮肤变化,因此在治疗期间必须仔细监测.其在有机溶剂中的溶解性和水溶解性有限是显著的物理特性,影响其配方和行政管理途径.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

2-n-butyl 3-(4-methoxy benzoyl)-benzofuran 2-chloro-N,N-diethylethylamine hydr°Chloride 2-n-butyl-3-(3',5'-diiodo-4'-hydroxybenzoyl)benzofuran 1-(4-methoxyphenyl)-1,3-heptanedionedesethylamiodarone Didesethylamiodarone Deiodoamiodarone 2-n-butyl-3-(3-iodo-4-hydroxybenzoyl)-benzofuran

合成工艺路线路线简述

  • 合成目标产物 Amiodarone 主要起始原料 4'-Methoxyacetophenone
  • (文献来源)合成步骤主要原料 4'-Methoxyacetophenone
1-(4-甲氧基-苯基)-庚烷-1,3-二酮置于aluminum (III) Chloride,N-溴代丁二酰亚胺(Nbs),碘,三溴化硼,Potassium Carbonate,Sodium Iodide,Sodium Hydroxide体系中,用 甲醇,硝基甲烷,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 21.0H,反应生成胺碘酮
参考文献:Lewis酸催化的丙烯醛二聚体和1,3-二羰基化合物合成苯并呋喃和4,5,6,7-四氢苯并呋喃
标题:Lewis酸催化的丙烯醛二聚体和1,3-二羰基化合物合成苯并呋喃和4,5,6,7-四氢苯并呋喃
摘要:N-溴代琥珀酰亚胺为氧化剂,由丙烯醛二聚体和1,3-二羰基化合物合成2,3-二取代苯并呋喃.该方法用于合成两个商业药物分子,苯溴马隆和胺碘酮.所提出的反应机理涉及使用路易斯酸催化剂的n-溴琥珀酰亚胺(nbs)辅助的自动串联催化.为了证明所提出的机理,成功地分离了中间体,该中间体可以转化为4,5,6,7-四氢苯并呋喃.
Doi:10.1021/acs.Joc.9B00270

海关参考信息

专利信息


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-9890132-B2
优先权日:2013-08-25
标 题 :Process for the preparation of anti-inflammatory aroylbenzofuran compounds
发明人:RAMANA CHEPURI VENKATA; KOMMAGALLA YADAGIRI; SRINIVAS KOLLURU
权利人:COUNCIL SCIENT IND RES; COUNCIL SCIENT IND RES
摘要:Disclosed herein an efficient process for synthesis of benzofuran analogs having anti-inflammatory activity which comprises, Ru-catalyzed branched and linear selective alkylation of aroylbenzofurans formula-I with alpha, beta unsaturated esters of formula-II via C—H activation in presence of base, additives and organic solvent at suitable temperature to give high yield of desired linear alkylated benzofuran compounds of formula-III or branched alkylated benzofuran compounds of formula-IV or mixture thereof.

专利号:US-9982008-B2
优先权日:2012-06-19
标题 :Preparation and uses of obeticholic acid
发明人:STEINER ANDRÉ; WAENERLUND POULSEN HEIDI; JOLIBOIS EMILIE; REWOLINSKI MELISSA; GROSS RALF; SHARP EMMA; DUBAS-FISHER FIONA; EBERLIN ALEX
权利人:INTERCEPT PHARMACEUTICALS INC
摘要:The present invention relates to obeticholic acid: n nor a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

专利号:US-11033889-B2
优先权日:2018-10-23
标 题:Palladium acyclic diaminocarbene complexes as precatalysts for Hiyama coupling and the tandem one-pot fluoride free Hiyama coupling/cyclization for the synthesis of biologically relevant
发明人:SINGH CHANDAN; GHOSH PRASENJIT
权利人:INDIAN INST TECHNOLOGY BOMBAY
摘要:The present invention provides Acyclic diaminocarbene complex of formula (I):Wherein,M is palladium;X is monoanionic ligand selected from Cl, Br or I;Where R1 is different from R2;R1 is selected from the group consisting of alkyl or aryl, each of which have 4 to 20 carbon atoms, and may optionally contain one or more heteroatoms;R2 is selected from the group consisting of alkyl, or aryl each of which have 4 to 20 carbon atoms, and may optionally contain one or more heteroatoms. The said palladium diamino carbine complex of the present invention are particularly useful as catalyst from Hiyama cross-coupling reaction.

专利号:US-4230624-A
优先权日:1977-09-02
标 题 :Process for the synthesis of derivatives of the benzofuran, chromene and isochromene type
发明人:LE CORRE MAURICE; HERCOUET ALAIN; BEGASSE BEATRICE
权利人:ANVAR
摘要:The invention relates to a process for the production of therapeutic compounds of the benzofuran, chromene and isochromene type of the general formula; in which formula, R1 and R3=H, lower alkyl, aralkyl or cycloalkyl R2=H or an organic radical and when D= R1 and R3 may represent an organic radical. The process comprising the cyclization in the liquid phase and in the presence of a base a compound of the formula; in which formula; R'=an alkyl, aryl or aralkyl radical and X-=an anion.

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.
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主要参考文献


1: Lee HC, Lo HC, Lo DM, Su MY, Hu JR, Wu CC, Chang SN, Dai MS, Tsai CT, Tsai HJ. Amiodarone Induces Overexpression of Similar to Versican b to Repress the EGFR/Gsk3b/Snail Signaling Axis during Cardiac Valve Formation of Zebrafish Embryos. PLoS One. 2015 Dec 9;10(12):e0144751. doi: 10.1371/journal.pone.0144751. eCollection 2015. [Epub ahead of print] Review. doi: 10.15283/ijsc.2015.8.2.170.
5: Elikowski W, Małek M, Skowroński M, Wróblewski D, Skrzywanek P, Zawilska K. [Hemoptysis during concomitant treatment with rivaroxaban and amiodarone in a patient with a history of pulmonary disease]. Pol Merkur Lekarski. 2015 Oct;39(232):227-30. Polish. doi: 10.1085/jgp.201511470. Epub 2015 Nov 16.
8: Witkowski M, Mochmann HC, Rauch U, Knie W, Landmesser U, Skurk C. Acute Thrombotic Occlusion of the Left Brachial Artery After Intra-Arterial Administration of Amiodarone. Crit Care Med. 2015 Nov 13. [Epub ahead of print] doi: 10.1155/2015/182154. Epub 2015 Oct 19.

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:10.1254/fpj.135.59
摘要:Kumagai K. [Upstream approach for atrial fibrillation]. Nihon Yakurigaku Zasshi. 2010 Feb;135(2):59–61. doi: 10.1254/fpj.135.59.
参考文献:10.1007/s10072-010-0218-4
摘要:Fröhlich I, Pilloy W, Vaillant M, Diederich NJ. Myocardial MIBG scintigraphy: a useful clinical tool : A retrospective study in 50 parkinsonian patients. Neurol Sci. 2010 Jun;31(3):403–6. doi: 10.1007/s10072-010-0218-4.
参考文献:10.1186/2047-783x-14-s4-259
摘要:Zielonka T, Demkow U, Zycinska K, Filewska M, Bialas B, Kus J, Radzikowska E, Remiszewski P, Szopinski J, Soszka A, Wardyn K, Skopinska-Rozewska E. Angiogenic activity of sera from interstitial lung disease patients in relation to clinical and radiological changes. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):259. doi: 10.1186/2047-783x-14-s4-259.
参考文献:10.1111/j.1442-200x.2009.02993.x
摘要:Tsuda E, Matsuo M, Sakaguchi H, Hayashi T, Hosoda K, Miyazaki A. Combined amiodarone and low-dose carvedilol treatment for severe heart failure in childhood. Pediatr Int. 2010 Feb;52(1):e39–42. doi: 10.1111/j.1442-200x.2009.02993.x.
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