CAS: 57526-81-5; Prenalterol

该化合物是一种合成化合物,被归类为乙型肾上腺素激动剂,主要用于治疗某些心血管病,特别是其刺激乙型-1肾上动反应受体的能力,导致心率和耐受性增加;该化合物的特征特征是其手性性质,其"(-)"标志表明其特定的立体化学作用,这对生物活动至关重要. (-)- 前体醇的半衰期相对较短,并在肝脏中新陈代谢,影响其药理动力学.该化合物通常在临床环境中施用,其功效可能受到剂量和个人病人反应等因素的影响.此外,(- )- 前肾色素可能对乙型动物具有共同的副作用,包括潜在的心血管影响,如心血管心动或心动反应.其化学结构包括一个苯性组和一个顺流体链,有助于其与肾上...

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合成工艺路线路线简述

    📜3-(4-甲氧基苯氧基)-1,2-丙二醇置于水,氢溴酸,三苯基膦,偶氮二甲酸二乙酯体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 31.5H,反应生成 丙胺酚醇
    参考文献:Effective Synthesis Of Non-Racemic Prenalterol Based On Spontaneous Resolution Of 3-(4-Hydroxyphenoxy)Propane-1,2-Diol
    标题:Effective Synthesis Of Non-Racemic Prenalterol Based On Spontaneous Resolution Of 3-(4-Hydroxyphenoxy)Propane-1,2-Diol
    摘要:Spontaneous Resolution Of Rac-3-(4-Hydroxyphenoxy)Propane-1,2-Diol Has Been Successfully Used In The Synthesis Of Both Enantiomers Of Chiral Drug Prenalterol.
    DOI:10.1016/j.Mencom.2019.03.028

    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-4777293-A
    优先权日:1984-08-13
    标题 :Method for the synthesis of pharmacologically active compounds and intermediates for such synthesis
    发明人:LAMM BO R
    权利人:HAESSLE AB
    摘要:A process for the preparation of an aryloxypropanolamine of the formula n n Ar--OCH.sub.2 CH(OH)CH.sub.2 NH--R I n n wherein Ar is a carbocyclic or heterocyclic aromatic group and R is an alkyl or substituted alkyl group having 1 to 6 carbon atoms, characterized in subjecting a compound of the formula ##STR1## to oxidative cleavage to a dialdehyde of the formula ##STR2## which is then made subject to reduction, amination, acetal hydrolysis, and, where required, removal of a nitrogen protective group, to the formation of a compound of formula I, or an acid addition salt thereof, a compound of formula II and the preparation thereof from mannitol.

    专利号:US-8017776-B2
    优先权日:2003-07-15
    标题 :Methods for synthesis of acyloxyalkyl compounds
    发明人:BHAT LAXMINARAYAN; GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

    专利号:US-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:US-8143437-B2
    优先权日:2002-02-19
    标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
    发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
    权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
    摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

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    主要参考文献

    1. Kendall MJ, Goodfellow RM, Westerling S. Prenalterol--a new cardioselective inotropic agent. J Clin Hosp Pharm. 1982 Jun;7(2):107-18. doi: 10.1111/j.1365-2710.1982.tb01010.x. 33(6):859-67. doi: 10.1097/00005344-199906000-00005.

    合成参考文献


    参考文献:10.1111/j.1399-6576.1980.tb01495.x
    摘要:Reiz S, Friedman A. Hemodynamic and cardiometabolic effects of prenalterol in patients with gram negative septic shock. Acta Anaesthesiol Scand. 1980;24(1):5–10. doi: 10.1111/j.1399-6576.1980.tb01495.x.
    参考文献:10.1007/bf02772206
    摘要:Walle T, Eaton EA, Walle UK, Pesola GR. Stereoselective metabolism ofRS-albuterol in humans. Clinical Reviews in Allergy & Immunology. 1996 Mar;14(1):101–13. doi: 10.1007/bf02772206.
    参考文献:10.1007/bf02942789
    摘要:Taylor A, Phelan D, McCarthy JR. Pain relief following cardiac surgery: A review. Irish Journal of Medical Science. 1996 Jan;165(1):1–6. doi: 10.1007/bf02942789.
    参考文献:10.1007/s002329900538
    摘要:Wangemann P, Liu J, Shimozono M, Scofield MA. Beta1-adrenergic receptors but not beta2-adrenergic or vasopressin receptors regulate K+ secretion in vestibular dark cells of the inner ear. J Membr Biol. 1999 Jul 01;170(1):67–77. doi: 10.1007/s002329900538.
    参考文献:10.1021/jm00152a017
    摘要:Linschoten MR, Bultsma T, IJzerman AP, Timmerman H. Mapping the turkey erythrocyte beta receptor: a distance geometry approach. J Med Chem. 1986 Feb;29(2):278–86. doi: 10.1021/jm00152a017.
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