CAS: 1086026-31-4; (S)-3-(3-(((3,4-Dimethoxybicyclo[4.2.0]Octa-1,3,5-Trien-7-yl)Methyl)(Methyl)Amino)Propyl)-7,8-Dimethoxy-1H-Benzo[d]Azepin-2(3H)-One

该化合物是一种化学化合物,主要以其在心血管药理学中的角色著称,主要以它的作用而著称,它是一种作为ivabradine衍生物的化学化合物,其特点是它能够有选择地抑制超极化活化的循环核酸化(HCN)渠道,特别是HCN4,它在控制心率方面起着关键作用.该化合物通常用于研究环境,以探索其对心脏病和腹肌等条件的潜在治疗影响.结构上,脱水ivabradine与母体化合物相比,具有一种经修改的化学框架,这可能会影响其药效,安全性特征和潜在副作用.该化合物经常被研究其功效,安全性以及潜在副作用,有助于理解心率调制.与许多制药化合物一样,其溶性,稳定性以及与生物系统的互动是决定其在临床环境中适用性的关键特征.

结构式图片

上下游产品

[{(7S)-3,4-dimethoxybicyclo[4.2.0]°Cta-1,3,5-trien-7-yl}methyl](methyl)amine 7,8-dimethoxy-3-[3-iodopropane]-1,3-dihydro-2H-3-benzazepin-2-one 3-{3-[[(3,4-Dimethoxybicyclo[4.2.0]°Cta-1,3,5-trien-7-yl)methyl]-(methyl)amino]propyl}-7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one 1-[(7S)-3,4-dimethoxybicyclo[4.2.0]°Cta-1,3,5-trien-7-yl]-N-methylmethanamine hydr°Chloride ivabradine ivabradine hydr°Chloride

合成工艺路线路线简述

    Ethyl ((3,4-Dimethoxybicyclo[4.2.0]octa-1,3,5-Trien-7-yl)Methyl)Carbamate置于lithium Aluminium Tetrahydride,Sodium Hydroxide体系中,用 四氢呋喃,乙醇,乙酸乙酯 用作溶剂,化学反应 19.5H,反应生成去氢伊伐布雷定
    参考文献:Process For The Synthesis Of (2E)-3-(3,4-Dimethoxyphenyl)Prop-2-Enenitrile,And Application In The Synthesis Of Ivabradine And Addition Salts Thereof With A Pharmaceutically Acceptable Acid
    标题:Process For The Synthesis Of (2E)-3-(3,4-Dimethoxyphenyl)Prop-2-Enenitrile,And Application In The Synthesis Of Ivabradine And Addition Salts Thereof With A Pharmaceutically Acceptable Acid
    摘要:化合物(i)的合成过程:在伊维布地定的合成中的应用,以及其与药用可接受酸的加合盐和水合物.

    专利信息


    专利号:US-8927708-B2
    优先权日:2013-03-26
    标 题 :Process for the synthesis of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one compounds, and application in the synthesis of ivabradine
    发明人:LE FLOHIC ALEXANDRE
    权利人:SERVIER LAB
    摘要:Process for the synthesis of the compound of formula (I): n nwherein R represents a para-methoxybenzyl (PMB) group or the following group:n n nApplication in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

    专利号:US-8779122-B2
    优先权日:2012-11-08
    标 题:Process for the synthesis of (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
    发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC
    权利人:SERVIER LAB
    摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

    专利号:WO-2019202611-A1
    优先权日:2018-04-21
    标题:An improved process for the synthesis of ivabradine and its pharmaceutically acceptable salts
    发明人:NANDEPU Venkateswara Rao; BOPPANA DURGA PRASAD
    权利人:METROCHEM API PVT
    摘要:: Disclosed herein is an improved process for the preparation of Ivabradine and pharmaceutically acceptable salts thereof. The invention more particularly disclosesthe synthesis of key intermediates viz.,(S)-N-[(4,5-dimethoxybenzocydobut-l-yl)-methyl]-N- (methyl)amine hydrochloride of Formula-II and 3-(3-Iodopropyl)-7,8-dimethoxy-1,3-dihydro-2H-3-benzapin-2-one of Formula-III, and its use in industrial synthesis of Ivabradine and pharmaceutically acceptable salts thereof.

    专利号:US-8859763-B1
    优先权日:2013-05-17
    标题 :Process for the synthesis of 3,4-dimethoxybicyclo[4.2.0]OCTA-1,3,5-triene-7-carbonitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
    发明人:VAYSSE-LUDOT LUCILE; LE FLOHIC ALEXANDRE; VAULTIER MICHEL; PUCHEAULT MATHIEU; KAMINSKI THOMAS
    权利人:SERVIER LAB
    摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

    专利号:US-8779123-B2
    优先权日:2012-12-06
    标题:Process for the synthesis of 3-(2-bromo-4,5-dimethoxyphenyl)propanenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
    发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC
    权利人:SERVIER LAB
    摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

    专利号:US-8779121-B2
    优先权日:2012-10-12
    标题:Process for the synthesis of 3-(2-bromo-4,5-dimethoxyphenyl)propanenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
    发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC
    权利人:SERVIER LAB
    摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
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    主要参考文献

    参考标题:Process For The Synthesis Of 3-(2-Bromo-4,5-Dimethoxyphenyl)Propanenitrile, And Application In The Synthesis Of Ivabradine And Addition Salts Thereof With A Pharmaceutically Acceptable Acid
    摘要:Process For The Synthesis Of The Compound Of Formula (I): Application In The Synthesis Of Ivabradine, Addition Salts Thereof With A Pharmaceutically Acceptable Acid And Hydrates Thereof.

    合成参考文献


    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2006).
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