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。
Abstract
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 1H-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.
关键词
溴他西尼 /
合成
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Key words
bretazenil /
synthesis
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李立威;程志刚;马学功.
溴他西尼的合成[J]. 中国药学杂志, 2008, 43(16): 1275-1277
LI Li-wei;CHENG Zhi-gng;M Xue-gong.
Synthesis of Bretazenil [J]. Chinese Pharmaceutical Journal, 2008, 43(16): 1275-1277
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参考文献
[1] TASHMA 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.
[2] NUTT D J. Alcohol alternativesa goal for psychopharmacology[J] . J Psychopharmacol，2006，20(3)： 318-320.
[3] MAGDEN W H， REINACH E K. Diazepine derivatives. US435 3827，USA，4353827[P] .1982-10-12.
[4] KATSIFIS A G，MCPHEE M E，MATTNER F，et al. Synthesis of 123I-labelled analogues of imidazobenzodiazepine receptor ligands[J] . Aust J Chem，1999，52(11)：1061-1069.
[5] TOKUNAGA 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.
[6] POLYCHRONOPOULOS 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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脚注
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