CAS: 56341-08-3; Mabuterol
该化合物是一种合成化合物,被归类为乙型抗艾激动剂,主要用于支气管消毒功能,用于治疗哮喘和慢性阻塞性肺病等呼吸状况.它的作用是刺激气管滑动肌肉中的乙-2肾上激素受体,导致支气管通过放松和放大,从而方便呼吸.Mabuterol的特点是对β-2受体采取相对有选择性的行动,最大限度地减少通常与非选择性乙型激动剂相关的心血管副作用.该化合物通常通过吸入方式施用,以便在肺部中实现局部影响,同时减少系统性接触.其药用植物学学学作用包括快速行动,使其适合支气管的急性减压.与其他乙型激动剂一样,潜在的副作用可能包括激素,呼吸道和心率上升,特别是在较高剂量的情况下.
- 英文名称Mabuterol
- 中文名称马布特罗
- IUPAC名称4-Amino-alpha-((tert-butylamino)methyl)-3-chloro-5-(trifluoromethyl)benzyl alcohol
- 其它别名(?à)-Mabuterol; Ambuterol; Mabuterol
- CAS编号56341-08-3
- MFCD编号:MFCD00867035
- FDA UNII编号:R4K19W6S7Q
- 分子式:C13H18ClF3N2O分子量:310.747
- 产品CID: 1536682
- 同类组份化合物CAS56341-08-3 (free base)54240-36-7 (HCl)
- 产品分类原料药 → 呼吸系统用药 → 平喘药
物理性质
- 熔点85-87 °C
- 沸点375.9 °C at 760mmHg
- 闪点181.1 °C
- 密度1.278g/cm3
- pKa:13.37±0.20(预测)
- PSA:58.28
- LogP:4.3346
- 折射率1.516
- 蒸汽压2.57E-06 mmHg at 25 °C
- 溶解性DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml
- 外观形态白色至类白色结晶性固体
- 储存条件Hygroscopic,-20°CFreezer,UnderInertAtmosphere
- 产品应用马布特罗(56341-08-3)的用途:β2-受体兴奋剂,有支气管扩张和抗过敏作用,可降低痰的黏度,增加纤毛输送痰液的速度,对变应原所致的皮肤反应有抑制作用.用于支气管哮喘,慢性支气管炎,肺气肿,气道阻塞性疾病等,可缓解这些疾病引起的呼吸困难等症状.只需轻轻,
- 性质描述马布特罗(56341-08-3)的性状:1.DL-盐酸马布特罗(Mabuterol Hydr°Chloride):C13H18ClF3N2O・HCl.从乙酸乙酯-乙醚结晶,熔点105～20.6°C(分解).易溶于水.急性毒性LD50雄,雌小鼠,雄,雌大鼠(mg/kg):220.8,199.9,319.3,305.6口服;41.5,51.1,26.4,28.1静脉注射;113.0,125.7,117.2,123.1皮下注射;60.3,60.0,76.3,78.3腹腔注射.急性毒性LD50雄,雌兔(mg/kg):284,243口服;19,18静脉注射.2.D-构型盐酸盐:熔点＞194°C(缓慢分解).[α]20364＋154.9°(c=1,甲醇).3.L-构型盐酸盐:熔点＞194°C(缓慢分解).[α]20364－154.8°(c=1,甲醇).只需轻轻,
MSDS等安全信息
上下游产品
4'-amino-3'-chloro-5'-trifluoromethyl-2-tert.-butylamino-acetophenone 4'-amino-3'-chloro-5'-trifluoromethyl-acetophenone 1-[4-Amino-3-chloro-5-(trifluoromethyl)phenyl]-2-bromoethanoned-1-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-ethanol (S)-mabuterol (R)-mabuterol合成工艺路线路线简述
📜4'-Amino-3'-Chloro-5'-Trifluoromethyl-2-Tert.-Butylamino-Acetophenone置于sodium Tetrahydroborate体系中,用 异丙醇 作为反应溶剂,化学反应 4.0H,反应生成 马布台诺
参考文献:Kruger; Keck; Noll,Arzneimittel-Forschung/drug Research,1984,Vol. 34,# 11 A,P. 1612-1624
标题:Kruger; Keck; Noll,Arzneimittel-Forschung/drug Research,1984,Vol. 34,# 11 A,P. 1612-1624
海关参考信息
- 2902600000-乙苯
2903919090-氯苯
2906210000-苄醇
2922110001-单乙醇胺 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
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-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:WO-2009094569-A2
优先权日:2008-01-25
标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates
专利号:US-2005222431-A1
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
专利号:KR-101513003-B1
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy compositions and applications
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Song X, Zhao C, Dai C, Ren Y, An N, Wen H, Pan LI, Cheng M, Zhang Y. Suppression of the increasing level of acetylcholine-stimulated intracellular Ca(2+) in guinea pig airway smooth muscle cells by mabuterol. Biomed Rep. 2015 Nov;3(6):778-786. Epub 2015 Aug 4.
2: Lu X, Liu P, Chen H, Qin F, Li F. Enantioselective pharmacokinetics of mabuterol in rats studied using sequential achiral and chiral HPLC. Biomed Chromatogr. 2005 Nov;19(9):703-8. doi: 10.1002/jlcr.3446. Epub 2016 Oct 13.
17: Nakamura M, Yamaya M, Fukushima T, Sekizawa K, Sasaki H, Takishima T. Effect of mabuterol on tracheal mucociliary clearance of magnetized iron particles in anesthetized dogs. Respiration. 1991;58(1):33-6. Japanese.
合成参考文献
参考文献:10.1007/s00216-010-3484-3
摘要:Peters RJB, Oosterink JE, Stolker AAM, Georgakopoulos C, Nielen MWF. Generic sample preparation combined with high-resolution liquid chromatography–time-of-flight mass spectrometry for unification of urine screening in doping-control laboratories. Analytical and Bioanalytical Chemistry. 2010 Feb 16;396(7):2583–98. doi: 10.1007/s00216-010-3484-3.
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