CAS: 84379-13-5; Bretazenil

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上下游产品

CAS号2769-72-4 异氰基乙酸乙酯

合成工艺路线路线简述

  • 合成目标产物 Bretazenil 主要起始原料 1H-Pyrrolo[2,1-C][1,4]Benzodiazepine-5,11(10H,11Ah)-Dione, 6-Bromo-2,3-Dihydro-, (11As)-
  • (文献来源)合成步骤主要原料 1H-Pyrrolo[2,1-C][1,4]Benzodiazepine-5,11(10H,11Ah)-Dione, 6-Bromo-2,3-Dihydro-, (11As)-
📜(11As)-6-Bromo-1,2,3,11A-Tetrahydro-5H-Pyrrolo[2,1-C][1,4]Benzodiazepine-5,11(10H)-Dione置于potassium Tert-Butylate,Sodium Hydride体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 溴他西尼
参考文献:Synthesis Of 123I-Labelled Analogues Of Imidazobenzodiazepine Receptor Ligands.
标题:Synthesis Of 123I-Labelled Analogues Of Imidazobenzodiazepine Receptor Ligands.
摘要:溴代或碘代异丁烯酸酐与 N-甲基甘氨酸,L-脯氨酸或 D-脯氨酸反应,得到溴代或碘代的 1,4-苯并二氮杂环庚二酮. 或碘代的 1,4-苯并二氮杂环庚二酮,在与乙基或叔丁基异氰基乙酸酯缩合后 异氰基乙酸乙酯或异氰基乙酸叔丁酯缩合后,得到溴代或碘代咪唑苯并 碘咪唑并二氮杂卓羧酸酯.这些芳基卤化物 在(三苯基膦)存在下,用双(三丁基锡)将这些芳基卤化物转化为相应的三丁基锡烷. 三苯基膦)钯(0)的存在下,用双(三丁基锡)将这些芳基卤化物转化为相应的三丁基锡烷,然后用 在氯胺-T 的存在下,用(123I)碘化钠处理锡烷,得到所需的 123I 标记. 得到所需的 123I 标记的类似物 咪唑苯并二氮杂卓受体配体氟马西尼和溴他西尼.
DOI:10.1071/ch99135

海关参考信息

专利信息


专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

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✅ COA系统入驻 | 共享模式

主要参考文献


1: Licata SC, Rowlett JK. Self-administration of bretazenil under progressive-ratio schedules: behavioral economic analysis of the role intrinsic efficacy plays in the reinforcing effects of benzodiazepines. Drug Alcohol Depend. 2011 Jan 15;113(2-3):157-64. doi: 10.1016/j.drugalcdep.2010.07.019. Epub 2010 Aug 30.
2: Munro G, Lopez-Garcia JA, Rivera-Arconada I, Erichsen HK, Nielsen EØ, Larsen JS, Ahring PK, Mirza NR. Comparison of the novel subtype-selective GABAA receptor-positive allosteric modulator NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem, bretazenil, and gaboxadol in rat models of inflammatory and neuropathic pain. J Pharmacol Exp Ther. 2008 Dec;327(3):969-81. doi: 10.1124/jpet.108.144568. Epub 2008 Sep 12. Epub 2005 Dec 8. Epub 2005 Oct 19.
15: Acri JB, Serdikoff SL, Witkin JM, Sannerud CA. Discriminative stimulus effects of the benzodiazepine receptor partial agonist bretazenil in pigeons and in rats. Behav Pharmacol. 1996 Jan;7(1):72-77.

合成参考文献


参考文献:10.1016/j.bmcl.2012.11.066
摘要:Jackson A, Guilbert BB, Plant SD, Goggi J, Battle MR, Woodcraft JL, Gaeta A, Jones CL, Bouvet DR, Jones PA, O'Shea DM, Zheng PH, Brown SL, Ewan AL, Trigg W. The development of potential new fluorine-18 labelled radiotracers for imaging the GABA(A) receptor. Bioorg Med Chem Lett. 2013 Feb 01;23(3):821–6. doi: 10.1016/j.bmcl.2012.11.066.
参考文献:10.2165/00003088-199223030-00003
摘要:Mandema JW, Danhof M. Electroencephalogram effect measures and relationships between pharmacokinetics and pharmacodynamics of centrally acting drugs. Clin Pharmacokinet. 1992 Sep;23(3):191–215. doi: 10.2165/00003088-199223030-00003.
参考文献:10.1007/pl00005485
摘要:Bizot J, Le Bihan C, Puech AJ, Hamon M, Thiébot M. Serotonin and tolerance to delay of reward in rats. Psychopharmacology (Berl). 1999 Oct;146(4):400–12. doi: 10.1007/pl00005485.
参考文献:10.1007/s00441-006-0284-3
摘要:Möhler H. GABA(A) receptor diversity and pharmacology. Cell Tissue Res. 2006 Nov;326(2):505–16. doi: 10.1007/s00441-006-0284-3.
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