CAS: 13523-86-9; Pindolol

该化合物是一种非选择性乙型肾上腺素对抗物,通常用于治疗高血压和某些类型的焦虑性失调,其特点是能够阻截乙型-1和乙型-2肾上腺受体,这有助于降低心率和血压.平地醇具有中度脂肪溶解性,允许它穿过血液脑屏障,这可能会造成其不解作用.平地醇的化学结构包括一个凝固的环,这是其药理活动的一个关键特征.它一般是口服,其半衰期相对较短,需要全天多剂量才能产生持续治疗效果.平地醇还可能表现出内在的血压活动,这意味着它可以部分刺激乙型受体,同时堵塞它们,这可能导致心血管影响的独特特征.常见的副作用包括疲劳,眩晕和胃肠紊乱.与任何药物一样,病人咨询保健专业人员进行个性化咨询和监测也很重要.

结构式图片

欧盟法规

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CAS号76989-08-7 1-[1-(4-methylp... | CAS号76989-09-8 1-chloro-3-[1-(... | CAS号75-31-0 异丙胺 | CAS号81102-66-1 [2R]-3-(2-methy... | CAS号81102-65-0 (S)-2,2-dimethy... | CAS号81102-68-3 (S)-2-hydroxy-3... | CAS号81132-32-3 [2R]-(+)-1-isop... | CAS号74088-75-8 3-isopropyl-5-(... | CAS号81745-07-5 (E)-5-((2-(2-(d... | CAS号74088-78-1 3-isopropyl-5-(...

合成工艺路线路线简述

    📜1-氯-3-[1-(4-甲基苯基)磺酰基-4-吲哚氧基]-2-丙醇置于sodium Hydroxide,Lithium Iodide体系中,用 乙醇 用作溶剂,化学反应 36.0H,反应生成吲哚洛尔
    参考文献:Preparation Of Alkyl-Substituted Indoles In The Benzene Portion. Part 7. Synthesis Of (.+-.)-And (S)-(-)-Pindolol.
    标题:Preparation Of Alkyl-Substituted Indoles In The Benzene Portion. Part 7. Synthesis Of (.+-.)-And (S)-(-)-Pindolol.
    摘要:描述了一种新的短步合成β-肾上腺素能阻断剂心得安(1-(4-吲哚氧基)-3-(2-丙胺基)-2-丙醇)的方法.在酸催化下,4-[1-(4-甲基苯基)磺酰-3-吡咯基]-4-氧丁醛(14)与(+/-)-3-氯-1,2-丙二醇(12)和(R)-1-O-[(4-甲基苯基)磺酰]甘油(24)反应,得到(+/-)-1-氯-3-[1-(4-甲基苯基)磺酰-4-吲哚氧基]-2-丙醇(15)和(R)-(-)-3-[1-(4-甲基苯基)磺酰-4-吲哚氧基]-1-[(4-甲基苯基)磺酰氧基]-2-丙醇(25).这些化合物与异丙胺反应并除去吲哚氮上的保护基团,得到了(+/-)-和(S)-(-)-心得安(3和4),从而构成了从 Readily Available Aldehyde (14)出发的高效三步合成的3和4的合成方法.
    Doi:10.1248/cpb.40.2353

    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-10005720-B2
    优先权日:2013-04-05
    标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
    发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
    权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
    摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

    专利号:US-8026375-B2
    优先权日:2007-04-13
    标题:Transition metal catalyzed synthesis of N-aminoindoles
    发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; RKYEK OMAR; URMANN MATTHIAS; ALONSO JORGE
    权利人:SANOFI AVENTIS
    摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

    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.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Bickel J, Jungen H, Müller A, Szewczyk A, Ondruschka B, Iwersen-Bergmann S. Toxicologic analysis of 35 drugs in post mortem human blood samples with focus on antihypertensive and antiarrhythmic drugs. J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Jul 15;1242:124196. doi: 10.1016/j.jchromb.2024.124196. Epub 2024 Jun 10. 66(1703):81-88. doi: 10.58347/tml.2024.1703a. 10(9):e29979. doi: 10.1016/j.heliyon.2024.e29979.
    4: Wang J, Guo Z, Guo Y, Zhang Y, Yu P, Ye Z, Qian Y, Yoshimura C, Wang T, Zhang L. Photochemical fate of β-blocker pindolol in riverine and its downstream coastal waters. Sci Total Environ. 2024 Jun 1;927:172236. doi: 10.1016/j.scitotenv.2024.172236. Epub 2024 Apr 4.
    194:106472. doi: 10.1016/j.nbd.2024.106472. Epub 2024 Mar 12. 149(8):2363-2373. doi: 10.1039/d3an02051g. 21(4):1729-1744. doi: 10.1021/acs.molpharmaceut.3c01081. Epub 2024 Mar 7. 36(2):e23644. doi: 10.1002/chir.23644. 388(2):688-700. doi: 10.1124/jpet.123.001920. Erratum in: J Pharmacol Exp Ther. 2024 Mar 15;389(1):128. doi: 10.1124/jpet.123.001920err. 23(1):478. doi: 10.1186/s12872-023-03514-2.

    合成参考文献


    参考文献:10.2147/ndt.s19613
    摘要:Blier P, Briley M. The noradrenergic symptom cluster: clinical expression and neuropharmacology. Neuropsychiatr Dis Treat. 2011;7(Suppl 1):15–20.
    参考文献:10.2165/11592070-000000000-00000
    摘要:Watkins CC, Pieper AA, Treisman GJ. Safety considerations in drug treatment of depression in HIV-positive patients: an updated review. Drug Saf. 2011 Aug 01;34(8):623–39. doi: 10.2165/11592070-000000000-00000.
    参考文献:10.1017/s1461145711001027
    摘要:Alvarez E, Perez V, Dragheim M, Loft H, Artigas F. A double-blind, randomized, placebo-controlled, active reference study of Lu AA21004 in patients with major depressive disorder. Int J Neuropsychopharmacol. 2012 Jun;15(5):589–600.
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