CAS: 54063-54-6; 7-[3-[[2-(3,5-Dihydroxyphenyl)-2-Hydroxyethyl]Amino]Propyl]-1,3-Dimethylpurine-2,6-Dione

该化合物是一种选择性的β2-Adrenergic受体激动剂,主要用作气喘和慢性阻塞性肺病等呼吸状况的支气管病(COPD)的管理. 它的主要优势在于它的快速行动和长期性,从支气管中得到有效的缓解. Reproterol对β2-受体具有很高的特性,与非选择性的激动剂相比,最大限度地减少心血管的副作用. 化合物通常通过吸入进行局部投放,确保有针对性的治疗效果,同时减少系统接触. 它的药理学特征支持其在急性和保持治疗中的使用,在临床实践中提供效果和可耐性平衡.

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    合成工艺路线路线简述

      📜7-[3-[[4-[2-(3,5-Dihydroxyphenyl)-2-Oxoethyl]Phenyl]Methylamino]Propyl]-1,3-Dimethylpurine-2,6-Dione 反应生成 瑞普特罗
      参考文献:Klingler,K.-H.;Bickel,E.
      标题:Klingler,K.-H.;Bickel,E.

      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-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.

      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

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      ✅ COA系统入驻 | 共享模式

      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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