CAS: 50700-72-6; 1-((2S,3S,5S,10S,13S,16S,17R)-3,17-Diacetoxy-10,13-Dimethyl-2-(Piperidin-1-yl)Hexadecahydro-1H-Cyclopenta[a]Phenanthren-16-yl)-1-Methylpiperidin-1-Ium Bromide

2,16-双(哌啶-1-基)雄甾-3,17-二醇置于溶剂黄146,Lithium Bromide,Zinc(II) Chloride体系中,用 乙醚,丙酮 作为反应溶剂,化学反应 3.66H,反应生成 维库溴铵
参考文献:维库溴铵及其高级中间体:晶体学和光谱学研究
标题:维库溴铵及其高级中间体:晶体学和光谱学研究
摘要:维库溴铵 (Piperidinium,1-[(2β,3α,5α,16β,17β)-3,17-Bis(Acetyloxy)-2-(1-Piperidinyl)Androstan-16-Yl]-1-Methyl-,Bromide; Norcuron®) 自 1982 年投放市场以来,已作为神经肌肉阻滞剂广泛用于麻醉学实践.然而,仍然缺乏对其先进合成中间体的详细晶体学和 NMR 分析.因此,为了填补这一文献空白,维库溴铵从市售的 3β-羟基-5α-Androstan-17-One(表雄酮)开始制备,对传统合成程序进行了一些修改.仔细的 NMR 研究允许完全分配1 H,13 C 和15维库溴铵及其合成中间体的 N NMR 信号.2β,16β-Bispiperidino-5α-Androstane-3α,17β-Diol 是第一个在最终构型中携带所有立体中心的先进合成中间体的结构和立体化学表征,通过单晶
DOI:10.1016/j.Steroids.2021.108928

专利信息

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:WO-9964032-A1
优先权日:1998-06-08
标题 :Combinatorial synthesis of multibinding libraries
发明人：CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.

专利号:WO-0112817-A1
优先权日:1999-08-12
标题:Evolution and use of enzymes for combinathorial and medicinal chemistry
发明人：KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
权利人:MAXYGEN INC; LIU LU; KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
摘要:This invention provides libraries of recombinant derivatizing enzymes that are useful for biocatalytic synthesis of derivatives oforganic molecules, including lead compounds for pharmaceutical use. The recombinant derivatizing enzymes catalyze reactions such as modification or replacement of functional groups on the organicmolecules, or addition of chemical moieties onto preexisting functional groups. The use of recombinant enzyme libraries enables one to obtain enzymes that catalyze the formation of organic molecule derivatives that could not otherwise be made using only naturally occurring enzymes.

专利号:US-7579461-B2
优先权日:2004-01-15
标题:Processes for the preparation of rocuronium bromide and intermediates thereof
发明人：ADAR ELIEZER; SONDACK DAVID; FRIEDMAN ODED; MANASCU IOSEF; FIZITZKI TAMIR; FREGER BORIS; ARAD ODED; WEISMAN ALEXANDER; KASPI JOSEPH
权利人:CHEMAGIS LTD
摘要:A novel process for preparing (2β,3α,5α,16β,17β)-17-acetoxy-3-hydroxy-2-(4-morpholinyl)-16-(1-pyrrolidinyl) androstane, a known intermediate in the synthesis of the skeletal muscle relaxant rocuronium bromide, is disclosed.

专利号:WO-9925385-A1
优先权日:1997-11-17
标 题:A method of increasing nucleic acid synthesis with ultrasound
发明人：UNGER EVAN C; MCCREERY THOMAS; SADEWASSER DAVID
权利人:IMARX PHARMACEUTICAL CORP
摘要:The present invention is directed to a method of increasing nucleic acid synthesis in a cell comprising administering to the cell a therapeutically effective amount of ultrasound for a therapeutically effective time such that said administration of said ultrasound results in said increased nucleic acid synthesis. The nucleic acid sequence may comprise an endogenous sequence or an exogenous sequence.

专利号:US-2012232225-A1
优先权日:2009-08-26
标 题:Synthesis and isolation of dendrimer systems
发明人：BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL
权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)).