CAS: 141626-36-0; N-(2-Butyl-3-(4-(3-(Dibutylamino)Propoxy)Benzoyl)Benzofuran-5-yl)Methanesulfonamide

该化合物是一种主要用于管理审前纤维纤维化和审判性颤动的抗心律药物,是氨碘酮的衍生物,旨在提供类似的治疗效应,减少副作用.德龙酮的特点是能够延长心脏组织中的行动潜在持续时间和耐腐期,这有助于稳定心脏节奏.化学上,它被归类为苯并呋喃衍生物,含有多种功能组,包括碳基和乙醚.它的分子结构有助于其药理特性,使它能够阻塞包括钾,钠和钙渠道在内的各种离子渠道,并显示乙烷-肾内腺对抗.德龙素通常通过口服,与阿米诺酮相比半衰期相对较短,这可能影响到多斯康酮.必须指出,虽然无人机达酮在节律控制方面是有效的,但它在心脏病严重衰竭的患者或由于潜在不利影响而有重大肝功能障碍的患者身上是被侵入的.

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CAS号111-92-2 二正丁胺 | CAS号1912-32-9 甲烷磺酸丁酯 | CAS号627040-50-0 N-(3-(4-bromoph...

合成工艺路线路线简述

  • 合成目标产物 Dronedarone 主要起始原料 N-Butyl Methanesulphonate And Methanesulfonamide, N-[3-[4-(3-Aminopropoxy)Benzoyl]-2-Butyl-5-Benzofuranyl]-
  • (文献来源)合成步骤主要原料 N-Butyl Methanesulphonate 和 Methanesulfonamide, N-[3-[4-(3-Aminopropoxy)Benzoyl]-2-Butyl-5-Benzofuranyl]-
4-(3-Chloropropoxy)Benzoyl Chloride置于四丁基溴化铵,四氯化锡,碳酸氢钠,三乙胺,甲胺,Potassium Iodide体系中,用 二氯甲烷,水,N,N-二甲基甲酰胺,异丙醇,甲苯 用作溶剂,化学反应 18.5H,反应生成决奈达隆
参考文献:纯化的纯决奈达隆盐酸盐的改进的可扩展路线
标题:纯化的纯决奈达隆盐酸盐的改进的可扩展路线
摘要:通过2-(-2-丁基-1-苯并呋喃-5-基)-1 H-异吲哚-1,3(2 H)二酮(12)的friedel-Craft酰化反应,有效合成可得的决奈达隆盐酸盐(2)通过使用伊顿试剂代替诸如alcl 3或sncl 4的有害和有毒金属卤化物催化剂,已经开发出了具有高收率和高纯度的4-(3-氯丙氧基)苯甲酸(13).
Doi:10.1021/op300017V

海关参考信息

专利信息


专利号:US-11897827-B1
优先权日:2022-11-22
标 题 :Carbon isotope exchange mediated by vanadium complexes
发明人:BUKHRYAKOV KONSTANTIN
权利人:BUKHRYAKOV KONSTANTIN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
摘要:The subject invention provides catalytical compounds/complexes, compositions comprising such compound/complex, synthesis of the compounds/complexes, and methods of using such compounds/complexes as catalysts in, for example, carbon isotope exchange (CIE) on target bioactive molecules. Methods that allow CIE directly on drug candidates are of great importance to chemistry, biology, and medicine. Especially valuable are catalytic procedures that rely on a limited collection of available labeled materials. The instant method comprises converting a methyl group to terminal â•?CH2 utilizing transfer dehydrogenation catalysts to enable V-based olefin metathesis, followed by a hydrogenation step. The one-pot strategy allows the formal methylation/demethylation sequence and can be applied to an assortment of alkyl-containing compounds.

专利号:US-2012108828-A1
优先权日:2010-09-09
标题 :Synthesis of dronedarone and salts thereof
发明人:SATHE DHANANJAY GOVIND; PATIL SAMADHAN DAULAT; GAIKWAD UMESH DILIP; RAO MANTRIPRAGADA NARAYANA; SHINDE AJIT BHASKAR
权利人:SATHE DHANANJAY GOVIND; PATIL SAMADHAN DAULAT; GAIKWAD UMESH DILIP; RAO MANTRIPRAGADA NARAYANA; SHINDE AJIT BHASKAR; USV LTD B S D MARG
摘要:The present invention relates to a process for preparation of Dronedarone or pharmaceutically acceptable salts thereof. More particularly, the present invention provides a process for preparation of Dronedarone hydrochloride, without the isolation of Dronedarone base.

专利号:US-8536350-B2
优先权日:2010-02-23
标 题:Process for the manufacture of dronedarone
发明人:SADA MARA; NARDI ANTONIO; MAIORANA STEFANO
权利人:SADA MARA; NARDI ANTONIO; MAIORANA STEFANO; LABORATORIO CHIMICO INT SPA
摘要:The invention relates to a new process for the preparation of dronedarone and its salts, in particular a synthesis process which allows said compound and its salts to be obtained with good yields, high purity and in an industrially expedient manner; the invention also concerns a new synthesis intermediate.

专利号:US-9550000-B2
优先权日:2011-09-09
标题 :Compositions, methods, and systems for the synthesis and use of imaging agents
发明人:ROBINSON SIMON P; YU MING
权利人:ROBINSON SIMON P; YU MING; LANTHEUS MEDICAL IMAGING INC
摘要:The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

专利号:US-6828448-B2
优先权日:2000-12-11
标 题:Methanesulphonamido-benzofuran, preparation method and use thereof as synthesis intermediate
发明人:FINO NOEL; LEROY CORINNE
权利人:SANOFI SYNTHELABO
摘要:The invention relates to 2-butyl-5-(methanesulfonamido)benzofuran, its preparation and its use. n This compound is a synthesis intermediate, in particular for the preparation of dronedarone.

专利号:US-8779201-B2
优先权日:2007-10-02
标题 :Process for preparing benzofurans
发明人:EKLUND LARS
权利人:CAMBREX KARLSKOGA AB
摘要:There is provided a process for the preparation of a compound of formula (I), wherein R 1 , R 2 , R 3 , R 4 , X and Y are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone.
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主要参考文献


1: De Vecchis R, Ariano C. Effects of dronedarone on all-cause mortality and on cardiovascular events in patients treated for atrial fibrillation. A meta analysis of RCTs. Minerva Cardioangiol. 2018 Sep 26. doi: 10.23736/S0026-4725.18.04719-9. [Epub ahead of print] doi: 10.1155/2018/4737489. eCollection 2018.
3: Chilukoti RK, Lendeckel J, Darm K, Bukowska A, Goette A, Sühling M, Utpatel K, Peters B, Homuth G, Völker U, Wolke C, Scharf C, Lendeckel U. Integration of "omics" techniques: Dronedarone affects cardiac remodeling in the infarction border zone. Exp Biol Med (Maywood). 2018 Jul;243(11):895-910. doi: 10.1177/1535370218788517.
4: Baek IH. Dose proportionality and pharmacokinetics of dronedarone following intravenous and oral administration to rat. Xenobiotica. 2018 Sep

合成参考文献


参考文献:10.3109/07853890.2011.594808
摘要:Kozlowski D, Budrejko S, Lip GY, Mikhailidis DP, Rysz J, Raczak G, Banach M. Dronedarone: an overview. Ann Med. 2012 Feb;44(1):60–72. doi: 10.3109/07853890.2011.594808.
参考文献:10.1107/s1600536811011093
摘要:Shi YB, Liu KK, Xia S, He FF, Wang HB. Methyl 4-(3-chloro-prop-oxy)benzoate. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1052.
参考文献:10.1016/j.bbamem.2011.07.001
摘要:Zhang YH, Colenso CK, Sessions RB, Dempsey CE, Hancox JC. The hERG K+ channel S4 domain L532P mutation: Characterization at 37°C. Biochimica et Biophysica Acta (BBA) - Biomembranes. 2011 Oct;1808(10):2477–87. doi: 10.1016/j.bbamem.2011.07.001.
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