溴他西尼的合成

李立威;程志刚;马学功

中国药学杂志 ›› 2008, Vol. 43 ›› Issue (16) : 1275-1277.

中国药学杂志 ›› 2008, Vol. 43 ›› Issue (16) : 1275-1277.
论著

溴他西尼的合成

  • 李立威;程志刚;马学功
作者信息 +

Synthesis of Bretazenil

  • LI Li-wei1,CHENG Zhi-gang2*,MA Xue-gong2
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文章历史 +

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

Key words

bretazenil / synthesis

引用本文

导出引用
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

参考文献

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