CAS: 63659-18-7; Betaxolol

该化合物是主要用于治疗高血压和某些类型的青光眼的选择性乙型-1肾上腺激素对抗剂. 作为乙型阻塞剂类别的一员,它通过阻止肾上腺素对心脏乙型-1受体的抗体采取行动,导致心率和心脏输出下降,有助于降低血压. 贝塔克罗的特点是,它相对高度选择性地选择乙型-1受体对乙型-2受体的受体,使得它更不可能引起支气管限制,这是非选择性乙型阻塞剂的共同副作用. 该物质通常通过口服或作为一种眼科疗法施用,其药理功能受到吸收,分布,新陈代谢和排泄等因素的影响. 贝塔克罗以其有利的副作用特征著名,但和所有药物一样,它可能会对某些病人造成不良影响,包括疲劳,眩晕或胸腔心. 它的化学结构包括苯氧丙基激素胺细胞,有助于其药性特性.

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

CAS号75-11-6 二碘甲烷 | CAS号75-31-0 异丙胺 | CAS号63659-17-6 [[4-[2-(环丙基甲氧基)... | CAS号63659-15-4 1-benzyloxy-4-(... | CAS号61439-59-6 2-(4-苯甲氧基苯基)乙醇 | CAS号56441-69-1 4-(苄氧基)苯乙酸乙酯 | CAS号63659-16-5 4-[2-(环丙基甲氧基)乙基]苯酚 | CAS号93221-48-8 左倍他洛尔 | CAS号63659-19-8 盐酸倍他洛尔

合成工艺路线路线简述

    2-Phenyl-3-Isopropyl-5-[[4-[2-(Cyclopropylmethoxy)Ethyl]Phenoxy]Methyl]Oxazolidine置于异丙醇,盐酸,甲苯,White Solid体系中,用 异丙醇,盐酸 作为反应溶剂,化学反应 16.0H,以was Obtained (74% Crude Yield Of Betaxolol Base)的收率获得产物倍他索洛尔
    参考文献:Process For Preparing Substituted Phenol Ethers Via
    标题:Process For Preparing Substituted Phenol Ethers Via
    摘要:苯醚类化合物,例如1-[4-[2-(环丙基甲氧基)乙基]苯氧基]-3-[(1-甲基乙基)氨基]-2-丙醇,也称为贝他珂洛,其化学式为:##str1## 通过首先用环氧氯丙烷反应苯酚基,然后用异丙胺反应,制备所需的二级胺-羟基侧链,制备.这些步骤期间不需要保护醇基.然后,使用适当的醛(如苯甲醛)与二级胺-醇基团反应,形成噁唑烷环保护剂,同时扩展醇链.噁唑烷环保护剂可通过简单的酸水解去除.

    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-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    专利号:US-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    专利号:WO-9614060-A1
    优先权日:1994-11-04
    标题 :Use of receptor agonists to stimulate superoxide dismutase activity
    发明人:MARKLUND STEFAN L; STRAALIN PONTUS
    权利人:MARKLUND STEFAN L; STRAALIN PONTUS
    摘要:The present invention relates to the use of a substance for the manufacture of a composition for stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells. In particular, the invention relates to the use of a substance for the manufacture of a composition for prophylaxis or treatment of a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical. Further, the invention relates to a method for determining the effect of a substance with respect to stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells and to substances which have been selected by said method. Within the scope of the invention is a method of preventing, diminishing, controlling or inhibiting a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical in a patient who has been established to have a high risk of developing a such disease or disorder, or who has developed a such disease or disorder, the method comprising administering an effective amount of a substance which is capable of stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells.

    专利号:US-2008287407-A1
    优先权日:2003-12-10
    标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
    发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
    权利人:NITROMED INC
    摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
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    主要参考文献


    1: Heijl A, Leske MC, Bengtsson B, Hyman L, Bengtsson B, Hussein M; Early Manifest Glaucoma Trial Group. Reduction of intraocular pressure and glaucoma progression: results from the Early Manifest Glaucoma Trial. Arch Ophthalmol. 2002 Oct;120(10):1268-79. doi: 10.1080/08037051.2018.1423543. Epub 2018 Jan 8. Factors for glaucoma progression and the effect of treatment: the early manifest glaucoma trial. Arch Ophthalmol. 2003 Jan;121(1):48-56. doi: 10.1016/j.msec.2018.07.065. Epub 2018 Jul 24. Review. doi: 10.1097/IJG.0000000000000500. Review. doi: 10.1002/chir.23012. Epub 2018 Sep 7. doi: 10.2147/IJN.S162306. eCollection 2018.
    11: Huang Y, Tao Q, Hou D, Hu S, Tian S, Chen Y, Gui R, Yang L, Wang Y. A novel ion-exchange carrier based upon liposome-encapsulated montmorillonite for ophthalmic delivery of betaxolol hydrochloride. Int J Nanomedicine. 2017 Mar 2;12:1731-1745. doi: 10.2147/IJN.S122747. eCollection 2017.
    12: Okutucu M, Fındık H, Arslan MG. Direct and crossover effects of brinzolamide, betaxolol, and latanoprost on choroidal thickness. Cutan Ocul Toxicol. 2019 Jun;38(2):196-200. doi: 10.1080/15569527.2019.1575390. Epub 2019 Mar 1. doi: 10.2147/IJN.S146346. eCollection 2018.

    合成参考文献


    摘要:Yakuri to Chiryo. Pharmacology and Therapeutics., 18(Suppl
    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
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