CAS: 1082-57-1; Tramazoline

该化合物是一个主要用作热量分解剂的化学化合物,属于非碘化化合物,经常用于鼻腔喷雾,以缓解与过敏或冷等条件有关的鼻腔拥堵;在鼻腔关紧血管,导致肿胀和拥堵减少;Tramazoline的特点是行动迅速,效果持续时间较短;它通常通过内部途径进行,虽然有效,但长期使用可导致反弹拥挤现象,即流行性炎药物;该化合物一般具有良好的耐燃性,但潜在的副作用可能包括鼻腔肌肉的局部刺激或干燥;与任何药物一样,必须使用TROMAzoline作为指导,以尽量减少风险和尽量扩大治疗益处.

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40507-80-0 21571-05-1 57004-77-0

欧盟法规

ECHA物质C&L通报REACH预注册

合成工艺路线路线简述

    📜1-氨基四氢化萘,乙腈,4,5-二氢-1H-咪唑-2-磺酸置于sodium Hydroxide体系中,用 氯仿 用作溶剂,以29.5 Mg (14%)的收率获得曲马唑啉
    参考文献:Method For Reducing Or Maintaining Intraocular Pressure In The Mammalian
    标题:Method For Reducing Or Maintaining Intraocular Pressure In The Mammalian
    摘要:一种药物组合物,最好是眼科溶液或眼科悬浮液,用于治疗哺乳动物,包括人类,以减少或维持眼内压,其药理活性成分为以下化合物之一或多个:其中x为o,S或nh;N为整数,取值为0,1或2;当n为0时,R.Sub.1为具有1至6个碳原子的低碳链烷基,R.Sub.2为h或具有1至6个碳原子的低碳链烷基;当n为1或2时,R.Sub.1和r.Sub.2为亚甲基(ch.Sub.2),或亚甲基上取代有一个r.Sub.5基团,其中r.Sub.5为1至6个碳原子的低碳链烷基;R.Sub.3和r.Sub.4独立地为h或具有1至6个碳原子的低碳链烷基;R.Sub.6为h或具有1至6个碳原子的低碳链烷基.

    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-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-RE41998-E
    优先权日:1990-02-26
    标题 :Compositions and methods of treatment of sympathetically maintained pain
    发明人:CAMPBELL JAMES N
    权利人:ARCLON THERAPEUTICS INC
    摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

    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.

    专利号:US-2003138490-A1
    优先权日:2001-09-08
    标 题 :Synthesis and uses of polymer gel nanoparticle networks
    发明人:HU ZHIBING; LU XIHUA; GAO JUN; PONDER BILL C; JOHN JOHN ST; MORO DANIEL G
    摘要:Disclosed is a new class of nanostructured polymeric materials comprising polymer gel nanoparticles that are covalently bonded through functional groups on the surfaces of neighboring particles. These nanoparticles may be prepared as suspensions in an aqueous or, non-aqueous environment. These gels have two unique and different structural networks; the primary network comprises crosslinked polymer chains in each individual particle, while the secondary network is a system of crosslinked nanoparticles. Particular polymer gel nanoparticle network compositions disclosed herein may function as carriers for controlled delivery of pharmaceuticals or other chemical agents, gel sensors and other commercial applications.

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    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

    合成参考文献


    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
    参考文献:10.1007/bf00511400
    摘要:Kobinger W. Rudolf Buchheim lecture. Drugs as tools in research on adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol. 1986 Feb;332(2):113–23. doi: 10.1007/bf00511400.
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