CAS: 128470-16-6; Arbutamine

该化合物是一种合成的催化激素衍生物,主要用作心脏诊断程序中的药理压力剂,其主要优势在于它能够模拟锻炼对心脏的影响,使无法接受身体压力测试的病人具有宝贵的价值.阿布托胺作为β1-Adrenergy受体激动剂,心率上升,心肌萎缩,从而便利了在回声心动学或溢热扫描等成像研究期间发现冠动脉疾病.其受控和可预测的热动能反应能够准确评估心脏功能.该化合物通常在临床监督下静脉注射,以确保诊断评估期间的安全性和有效性.

结构式图片

合成工艺路线路线简述

    📜3,4-二(叔-丁基二甲基硅烷基氧基)苯甲醛置于palladium On Activated Charcoal,2,6-Bis((2R-(Dinaphthyl(Oh)C)Pyrrolidino)Me)-4-Mepheoh,Diethylzinc 盐酸,Lithium Aluminium Tetrahydride,氢气,N,N-二异丙基乙胺,氯磷酸二苯酯体系中,用 四氢呋喃,甲醇,乙醚,二氯甲烷 用作溶剂,化学反应 54.0H,反应生成阿布他明
    参考文献:配体结构对锌催化的亨利反应的影响.(-)-地巴胺和(-)-Arbutamine的不对称合成.
    标题:配体结构对锌催化的亨利反应的影响.(-)-地巴胺和(-)-Arbutamine的不对称合成.
    摘要:[反应:见正文]报道了用于不对称的羟醛和硝基羟醛(亨利)反应的双核锌催化剂的各种改性配体的合成.这些修饰的配体促进的催化对映体选择性硝基羟醛反应导致β-受体激动剂(-)-地巴胺和(-)-Arbutamine的有效合成.
    Doi:10.1021/ol020077N

    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-11053227-B2
    优先权日:2017-12-20
    标 题:Process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction and novel synthesis intermediates
    发明人:COLLI CORRADO; BERTOLINI GIORGIO; SADA MARA; GARIS FARIS; NISIC FILIPPO; BIANCHI ALDO; BIAGGI CINZIA; DI FABIO ROMANO; RONZONI SILVANO; BERTUOLO STEFANIA; PRANDI ADOLFO; MAIORANA STEFANO
    权利人:OLON SPA
    摘要:Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.

    专利号:US-11766432-B2
    优先权日:2018-07-27
    标题 :Cleavable conjugates of catechol compounds and water-soluble polymers and methods of treatment using the same
    发明人:BENTLEY MICHAEL; FANG ZHIHAO; WEIMER REBECCA; VIEGAS TACEY; MOREADITH RANDALL
    权利人:SERINA THERAPEUTICS INC
    摘要:Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.

    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:EP-3728618-A1
    优先权日:2017-12-20
    标题 :Process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction and novel synthesis intermediates

    专利号:US-2020385366-A1
    优先权日:2017-12-20
    标 题 :Process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction and novel synthesis intermediates

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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

    主要参考文献


    1: Zhao S, Li S. A co-module approach for elucidating drug-disease associations and revealing their molecular basis. Bioinformatics. 2012 Apr 1;28(7):955-61. doi: 10.1093/bioinformatics/bts057. Epub 2012 Jan 28. Polish. Review. Review. Erratum in: J Nucl Med 2002 Oct;43(10):1376. Review.

    合成参考文献


    参考文献:10.1093/eurheartj/16.suppl_m.24
    摘要:Armstrong WF, Bach DS. Clinical and diagnostic utility of arbutamine for cardiovascular stress testing during echocardiographic monitoring. Eur Heart J. 1995 Nov;16 Suppl M():24–7. doi: 10.1093/eurheartj/16.suppl_m.24.
    参考文献:10.1002/jps.2600810605
    摘要:Riviere JE, Williams PL, Hillman RS, Mishky LM. Quantitative Prediction of Transdermal Iontophoretic Delivery of Arbutamine in Humans with the in Vitro Isolated Perfused Porcine Skin Flap. Journal of Pharmaceutical Sciences. 1992 Jun;81(6):504–7. doi: 10.1002/jps.2600810605.
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