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溴他西尼的合成 被引量：3

Synthesis of Bretazenil
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摘要 目的研究溴他西尼的合成。方法以3-溴苯胺为起始原料,经过成环、氧化、扩环等反应得到目标产物。结果用该合成路线得到溴他西尼,纯度≥99%,结构经核磁共振氢谱确证,总收率为12.4%,高于文献报道收率(4.8%)。结论本合成方法具有反应条件温和、质量易控制、转化率高等优点。 OBJECTIVE To study the synthetic process for bretazenil. METHODS Bretazenil was synthesized from 3- bromoaniline by cyclization, oxidation and ring-enlargement reaction, etc, RESULTS The purity of the product was above 99%. The structure of bretazenil was verified by ^1 H-NMR, The overall yield was 12.4%, which was higher than reported yield （4. 8% ）. CONCLUSION It is proved to be a method with mild condition, high quality and good yield.
作者 李立威 程志刚 马学功
机构地区 荆门职业技术学院药学院 武汉百科药物开发有限公司
出处 《中国药学杂志》 CAS CSCD 北大核心 2008年第16期1275-1277,共3页 Chinese Pharmaceutical Journal
关键词 溴他西尼 合成 bretazenil synthesis
分类号 R916 [医药卫生—药学]
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参考文献6

  • 1TASHMA Z, RAVEH L, LIANI H, et al. Bretazenil, a benzodiazepine receptor partial agonist, as an adjunct in the prophylactic treatment of OP poisoning[ J]. J Appl Toxicol, 2001, 21 ( suppl 1) :115-119.
  • 2NUTT D J. Alcohol ahernativesa goal for psychopharmacology[J]. J Psychopharmacol, 2006, 20(3): 318-320.
  • 3MAGDEN W H, REINACH E K. Diazepine derivatives. US435 3827 ,USA, 4353827[ P]. 1982-10-12.
  • 4KATSIFIS A G, MCPHEE M E, MATFNER F, et al. Synthesis of ^123 I-labelled analogues of imidazobenzodiazepine receptor ligands[J]. Aust J Chem,1999,52( 11 ) :1061-1069.
  • 5TOKUNAGA T, HUME W E, UMEZOME T, et al. Oxindole derivatives as orally active potent growth hormone secretagogues [J]. J Med Chem, 2001, 44(26):4641-4649.
  • 6POLYCHRONOPOULOS P, MAGIATIS P, SKALTSOUNIS A L, et al. Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases [ J ]. J Med Chem, 2004,47 (4) :935-946.

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  • 1WINSKY-SOMMERER R. Role of GABAA receptors in the physiology and pharmacology of sleep[J]. European Journal of Neuroscience, 2009 29(9): 1779-1794.
  • 2HIBBS R E, GOUAUX E. Principles of activation and permeation in an anion-selective Cys-loop receptor[J]. Nature, 2011,474(7349): 54-60.
  • 3SEUTIN V, SCUVEE-MOREAU J, DRESSE A. Evidence for a non-GABAergic action of quaternary salts of bicuculline on dopaminergie neurons[J]. Neuropharmacology, 1998, 36(11/12): 1653-1657.
  • 4SEIJAS J A, V,ZQUEZ-TATO M E CARBALLIDO-REBOREDO R. Solvent-free synthesis of functionalized flavones under microwave irradiation[J]. The Journal of Organic Chemistry, 2005, 70(7): 2855-2858.
  • 5LAM P Y S, CLARK C G, LI R, et al. Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor xa inhibitors as novel anticoagulants[J]. Journal of Medicinal Chemistry, 2003, 46(21): 4405-4418.
  • 6STUK T L, ASSINK B K, BATES R C, et al. An efficient and cost-effective synthesis of pagoclone[J]. Organic Process Research & Development, 2003, 7(6): 851-855.
  • 7STERNBACH L H, FRYER R I, KELLER O, et al. Quinazolines and 1,4-benzodiazepines. X. nitro-substituted 5-phenyl-l,4-benzodiazepine derivatives[J]. J. Med. Chem, 1963, 6: 261-265.
  • 8MCDONOUGH J A, DURRWACHTER commercially viable elonazepam process[J] 1997, 1(4): 268-272 J R. Development of a Org. Process Res. Dev,.
  • 9DONOHUE S R, DANNALS R F. A concise and efficient synthesis of flumazenil and its precursor for radiolabeling with fluorine-18[J]. Tetrahedron Letters, 2009, 50(52): 7271-7273.
  • 10YIN W, MAJUMDER S, CLAYTON T, et al. Design, synthesis and subtype selectivity of 3,6-disubstituted beta-earbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse[J]. Bioorg. Meal. Chem, 2010, 18(21): 7548-7564.

引证文献3

中国药学杂志
2008年 第16期

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