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.
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.