CAS: 13392-18-2; Fenoterol

该化合物是一种选择性的乙-2肾上腺激动剂,主要用作治疗哮喘和慢性阻塞性肺病(COPD)的支气管. 它的作用是刺激气道滑动肌肉中的乙-2肾上腺受体,导致支气管通过放松和放大,从而改善气流. 通常通过吸入施药,允许有针对性地向肺部投递,减少系统性副作用. 该物质的特征是其行动较快的开始和持续时间可能因配方而异. 除了其支气管效应外, enotor还可能表现出一些抗炎的特性. 但是, 同其他 bea-agestist 一样, 它可能会产生副作用, 如颤动, 热和心率上升, 特别是在较高剂量的情况下. 它的化学结构包括一个苯酚类和异丙胺动物, 有助于其药效活动. enotomilyamimoist, 通常与其他药物一起使用, 以提高呼吸条件下的治疗功效.

结构式图片

欧盟法规

REACH注册ECHA物质

上下游产品

bis-(3-chloro-2-hydroxy-propyl)-cyclohexyl-amine (+/-)-1-chloro-3-cyclohexylamino-2-propanol cyclohexylamine(S,S)-(+)-Fenoterol (R,R)-(-)-Fenoterol

合成工艺路线路线简述

    📜氢溴酸非诺特罗 以 95/5/0.05,Ch3Cn Isopropanol Hnet2 用作溶剂,化学反应 0.21H,反应生成非诺特罗
    参考文献:Preparation Of (R,R)-Fenoterol And (R,R)-Or (R,S)-Fenoterol Analogues And Their Use In Treating Congestive Heart Failure
    标题:Preparation Of (R,R)-Fenoterol And (R,R)-Or (R,S)-Fenoterol Analogues And Their Use In Treating Congestive Heart Failure
    摘要:本公开涉及发现(R,R)-和(R,S)-芬特罗类似物,其在结合β2-肾上腺素能受体方面具有高度的效果.提供了这些类似物的示例化学结构.还提供了包括公开的(R,R)-芬特罗和芬特罗类似物的制药组合物,以及使用这些化合物和组合物治疗心脏疾病(如充血性心力衰竭)和肺部疾病(如哮喘或慢性阻塞性肺疾病)的方法.

    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-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    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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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Jozwiak K, Plazinska A, Toll L, Jimenez L, Woo AY, Xiao RP, Wainer IW. Effect of fenoterol stereochemistry on the β2 adrenergic receptor system: ligand-directed chiral recognition. Chirality. 2011;23 Suppl
    1:E1-6. doi: 10.1002/chir.20963. Epub 2011 May 26. Review.
    2: Kässner F, Hodder R, Bateman ED. A review of ipratropium bromide/fenoterol hydrobromide (Berodual) delivered via Respimat Soft Mist Inhaler in patients with asthma and chronic obstructive pulmonary disease. Drugs. 2004;64(15):1671-82. Review. Review. Review. Review. Norwegian. Review. Review. Review. Review. German. Review.

    合成参考文献


    摘要:Iyakuhin Kenkyu. Study of Medical Supplies., 15(1140), 1984
    参考文献:10.1007/bf00562619
    摘要:Gandar R, de Zoeten LW, van der Schoot JB. Serum level of ritodrine in man. European Journal of Clinical Pharmacology. 1980 Mar;17(2):117–22. doi: 10.1007/bf00562619.
    参考文献:10.1007/bf02772207
    摘要:Boulton DW, Fawcett JP. Enantioselective disposition of albuterol in humans. Clinical Reviews in Allergy & Immunology. 1996 Mar;14(1):115–38. doi: 10.1007/bf02772207.
    参考文献:10.1007/bf02284970
    摘要:Warnke K, Hildebrandt R, Günther K, Langen U, Gundert-Remy U. The pharmacokinetics of theβ2-adrenoceptor agonist fenoterol in healthy women. European Journal of Clinical Pharmacology. 1992 Dec;43(6):663–5. doi: 10.1007/bf02284970.
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