CAS: 118457-14-0; (1S)-1-[(2S)-6-Fluoro-3,4-Dihydro-2H-Chromen-2-Yl]-2-[[(2S)-2-[(2R)-6-Fluoro-3,4-Dihydro-2H-Chromen-2-Yl]-2-Hydroxyethyl]Amino]Ethanol

该化合物是一种选择性的乙型-1肾上腺受体阻塞器,主要用于治疗高血压和心脏衰竭,其特点是能够降低血压,降低心率和心心肌萎缩,从而降低心力输出.Nebivoololol由于血管阻塞器的性能,在乙型阻塞器中是独一无二的,因为其血管阻塞器具有刺激释放硝基氧化物的能力,导致内分泌功能的改善.该物质通常通过口服施用,具有有利的药理学特征,包括长的半衰期,允许每天服一次.Nebivoolol一般都具有良好的缓解作用,其副作用可能包括疲劳,头痛和眩晕,尽管它比非选择性的乙型阻塞器更不可能引起肠道紧张.其化学结构包括一个气管中心,导致不同的抗血酶,导致其药性效应.

结构式图片

欧盟法规

REACH注册C&L通报REACH预注册

上下游产品

nebivolol (R)-2-amino-1-[(S)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]ethanol (R)-2-[(R)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-hydroxyethyl-4-methylbenzenesulfonate (S)-2-[(R)-2,2-dimethyl-1,3-dioxolan-4-yl]-6-fluoro-2,3-dihydr°Chromen-4-onenebivolol hydr°Chloride DL-nebivolol hydr°Chloride α,α'-iminobis(methylene)bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] hydr°Chloride (R)-1-((R)-6-Fluoro-chroman-2-yl)-2-[(S)-2-((R)-6-fluoro-chroman-2-yl)-2-hydroxy-ethylamino]-ethanol; hydr°Chloride

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:WO-2013018053-A1
    优先权日:2011-08-02
    标题 :Process for the preparation of epoxides as intermediates for the synthesis of nebivolol
    发明人:CIPOLLONE AMALIA; D ANDREA PIERO; FATTORI DANIELA
    权利人:MENARINI INT OPERATIONS LU SA; CIPOLLONE AMALIA; D ANDREA PIERO; FATTORI DANIELA
    摘要:The present invention relates to a novel process of synthesis of epoxides, 6-fluoro-2- (oxiran-2-yl) chroman (Figure 1), intermediates for the synthesis of nebivolol, depicted in Scheme (1), enabling to obtain the above- mentioned epoxides in a racemic or semichiral form.

    专利号:US-10392361-B2
    优先权日:2016-01-21
    标题:Process for the synthesis of intermediates of Nebivolol
    发明人:BARTOLI SANDRA; MANNUCCI SERENA; GRISELLI ALESSIO; STEFANINI ALESSIO
    权利人:MENARINI INT OPERATIONS LUXEMBOURG SA
    摘要:The present invention relates to a novel process for the synthesis of the intermediate compounds constituted by chromanyl haloketones of formula III and 6-fluoro-2-(oxiran-2-yl)chromans of formula I. n The intermediates thus obtained can be used for the synthesis of Nebivolol.

    专利号:US-8785664-B2
    优先权日:2010-02-11
    标 题 :Process for the preparation of nebivolol
    发明人:BARTOLI SANDRA; CIPOLLONE AMALIA; FATTORI DANIELA
    权利人:MENARINI INT OPERATIONS LU SA
    摘要:The present invention relates to a novel process for the synthesis of Nebivolol product represented in Scheme (1), comprised of a reduced number of high-yield steps, and characterized by the kinetic resolution of the two epoxide pairs diastereoisomeric therebetween (mixture 1), allowing to avoid complex chromatographic separations.

    专利号:US-8487122-B2
    优先权日:2010-02-11
    标题 :Process for the preparation of nebivolol
    发明人:BARTOLI SANDRA; CIPOLLONE AMALIA; FATTORI DANIELA
    权利人:BARTOLI SANDRA; CIPOLLONE AMALIA; FATTORI DANIELA; MENARINI INT OPERATIONS LU SA
    摘要:The present invention relates to a novel process for the synthesis of Nebivolol product represented in Scheme (1), comprised of a reduced number of high-yield steps, and characterized by the kinetic resolution of the two epoxide pairs diastereoisomeric therebetween (mixture 1), allowing to avoid complex chromatographic separations.

    专利号:US-2011250454-A1
    优先权日:2010-04-09
    标 题:Preparation of nebivolol
    发明人:HALDAR PRANAB; GOLLA CHINA MALAKONDAIAH; SWAPNA AKULA; KUMAR KARRI VIJAYA; JAWLEKAR SUHAS; TUMMALA ARJUN KUMAR; PATRO DEEPALI; YARRAGUNTLA SESHA REDDY; RAMAKRISHNAN SRIVIDYA; CHIMALA VENKATA RAMANA REDDY
    权利人:HALDAR PRANAB; GOLLA CHINA MALAKONDAIAH; SWAPNA AKULA; KUMAR KARRI VIJAYA; JAWLEKAR SUHAS; TUMMALA ARJUN KUMAR; PATRO DEEPALI; YARRAGUNTLA SESHA REDDY; RAMAKRISHNAN SRIVIDYA; CHIMALA VENKATA RAMANA REDDY
    摘要:Processes for the synthesis of pharmacologically active 2,2-iminobisethanol derivatives, e.g., 2H-1-benzopyran-2 methanol-α,α′-iminobis(methylene)]bis-[6-fluoro-3,4-dihydro-[2R*[R*[R*(S*)]]]], and their pharmaceutically acceptable salts.

    专利号:US-9090922-B2
    优先权日:2010-11-30
    标题:Process for the preparation of nebivolol
    发明人:MAURO SANDRO; FATTORI DANIELA; D ANDREA PIERO; CIPOLLONE AMALIA; D ANDREA ENZO; ERCOLANO CARMELA
    权利人:MAURO SANDRO; FATTORI DANIELA; D ANDREA PIERO; CIPOLLONE AMALIA; D ANDREA ENZO; ERCOLANO CARMELA; MENARINI INT OPERATIONS LU SA
    摘要:The present invention relates to a novel process for the synthesis of the Nebivolol product depicted in Scheme 1, comprised of a reduced number of high-yield steps, and characterized by the enzymatic resolution of the chroman ester precursor.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Sander GE, Giles TD. Nebivolol and valsartan as a fixed-dose combination for the treatment of hypertension. Expert Opin Pharmacother. 2015 Apr;16(5):763-70. doi: 10.1517/14656566.2015.1020790. Review. doi: 10.1016/j.cjca.2014.03.003. Epub 2014 Mar 5. Review. doi: 10.2147/IBPC.S50954. eCollection 2014. Review.
    4: Patrascu N. Diastolic heart failure in hypertension: possible preventive benefits of nebivolol beyond lowering blood pressure. Maedica (Buchar). 2013 Sep;8(3):285-9. Review.
    5: DiNicolantonio JJ, Lavie CJ, Fares H, Menezes AR, O'Keefe JH. Meta-analysis of carvedilol versus beta 1 selective beta-blockers (atenolol, bisoprolol, metoprolol, and nebivolol). Am J Cardiol. 2013 Mar 1;111(5):765-9. doi: 10.1016/j.amjcard.2012.11.031. Epub 2013 Jan 4. Review. doi: 10.2147/VHRM.S20669. Epub 2012 Mar 13. Review.

    合成参考文献


    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2008).
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知