CAS: 23031-25-6; Terbutaline

该化合物是一种合成药物,主要用作治疗哮喘和其他呼吸状况的支气管,属于被称为乙-2肾上腺激动剂的药物类别,该类药物通过放松空气道的肌肉而发挥作用,从而便利呼吸.乙丁胺线的特点是它能够有选择地刺激乙-2肾上腺受体,导致小心血管影响最小的血管分裂.该物质通常通过吸入,口服片或亚皮注射方式施用,视临床情况而定.乙丁胺线的半衰期相对较短,可以迅速采取行动,从而对急性哮喘袭击有效.此外,它可能表现出一些抗炎的特性,尽管其主要功能是支气管.普通的副作用包括激素,紧张和心率上升,通常比较轻.与任何药物一样,必须在医疗监督下使用基丁膜线来有效管理可能的相互作用和抗逆作用.

结构式图片

欧盟法规

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上下游产品

3,5-dihydroxyacetophenone 2-bromo-1-(3,5-dihydroxyphenyl)ethan-1-one tert-butylaminetert-butylamine terbutaline hemisulfate (-)-Terbutaline (+)-Terbutaline

合成工艺路线路线简述

  • 合成目标产物 5-(1-Hydroxy-2-Tert-Butylamino-Ethyl)Benzene-1,3-Diol 主要起始原料 3,5-Dibenzyloxyacetophenone
  • (文献来源)合成步骤主要原料 3,5-Dibenzyloxyacetophenone
硫酸特布他林置于potassium Carbonate体系中,用 甲醇 用作溶剂,化学反应 2.0H,反应生成特布他林
参考文献:Rac-Terbutaline的对映选择性拆分和光学纯的r-Terbutaline盐酸盐作为一种有效的抗哮喘药的评价.
标题:Rac-Terbutaline的对映选择性拆分和光学纯的r-Terbutaline盐酸盐作为一种有效的抗哮喘药的评价.
摘要:特布他林为β 2用于治疗哮喘和慢性阻塞性肺病(copd)的治疗中肾上腺素能受体兴奋剂.在特布他林的两种异构体(tbt 2)中,R异构体是产生治疗效果的强效对映异构体,而s异构体则显示出副作用.在这项研究中,[r-Terbutaline盐酸盐([r-Tbh 6)通过从外消旋硫酸特布他林(手性拆分合成的外消旋-Tbs 1)99.9%对映体过量(ee)在非常好的总产率(53.6%).此外,R-Tbh 6雾化的溶液在bricanyl®,这是外消旋的特布他林市售产品的一半剂量制备和体外气雾剂的性能和在豚鼠体内抗哮喘效果评价通过.肺部分娩.从研究中可以明显看出,半剂量的r-Tbh 6雾化溶液具有与bricanyl®相似的非常好气雾特性和抗哮喘效果.
Doi:10.1002/chir.22846

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-2006167025-A1
优先权日:2004-12-22
标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs
发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.

专利号:US-11311505-B2
优先权日:2017-02-24
标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts
发明人:MARTIN ALAIN
权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.

专利号:US-5442118-A
优先权日:1994-04-22
标题 :Asymmetric synthesis of (R)- and (S)-arylethanolamines from iminoketones
发明人:GAO YUN; HONG YAPING; ZEPP CHARLES M
权利人:SEPRACOR INC
摘要:A method for the enantioselective reduction of an alpha -iminoketone to an alpha -aminoalcohol is disclosed. The method utilizes a borane reducing agent as the reducing agent and a chiral 1,3,2-oxazaborole as the catalyst. The method is applied to the synthesis of R-albuterol from methyl 5-acetylsalicylate in high yield and high optical purity.

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.
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主要参考文献


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合成参考文献


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参考文献:10.1186/1472-6750-10-12
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参考文献:10.1111/j.1440-1681.2011.05574.x
摘要:Head SI, Ha TN. Acute inhibitory effects of clenbuterol on force, Ca2+transients and action potentials in rat soleus may not involve the β2‐adrenoceptor pathway. Clin Exp Pharma Physio. 2011 Aug 26;38(9):638–46. doi: 10.1111/j.1440-1681.2011.05574.x.
参考文献:10.1155/2011/917015
摘要:López E, Zafra MP, Sastre B, Gámez C, Fernández-Nieto M, Sastre J, Lahoz C, Quirce S, Del Pozo V. Suppressors of Cytokine Signaling 3 Expression in Eosinophils: Regulation by PGE2and Th2 Cytokines. Clinical and Developmental Immunology. 2011;2011():1–11. doi: 10.1155/2011/917015.
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