抗2型糖尿病药西他列汀杂质A的合成研究
发布时间：2018-11-15 07:43
【摘要】：目的合成西他列汀杂质A。方法将2,4,5-三氟苯乙酸、米氏酸和3-三氟甲基-5,6,7,8-四氢-1,2,4-三唑[4,3-α]吡嗪盐酸盐以"一锅法"反应得到中间体1-{3-三氟甲基-5,6-二氢-1,2,4-三唑并[4,3-a]吡嗪-7(8H)-基}-4-(2,4,5-三氟苯基)-1,3-丁二酮,再经硼氢化钠还原得到西他列汀杂质A。结果目标化合物的结构经IR、MS和1H-NMR确证。结论该方法未见文献报道,具有成本低、操作简单、反应温和、收率高等优点。
[Abstract]:Objective to synthesize the impurity A of citaletine. Methods the intermediate 1- {3- trifluoromethyl-56-dihydro-1H _ 1H _ 2H _ 2H _ 3H _ 3H _ 3H _ 3H _ 2H _ 3H _ 2H _ 2H _ 2H _ 2H _ 2H _ 2H _ 2H _ 1H _ 1H _ 1H _ 2 was obtained by one-pot reaction. 4-triazolo-7 (8H) -yl} -4- (2o 4N 5- trifluorophenyl) -1H 3-butanedione was reduced by sodium borohydride to obtain the impurity A. Results the structure of the target compound was confirmed by IR,MS and 1H-NMR. Conclusion the method has the advantages of low cost, simple operation, mild reaction and high yield.
【作者单位】： 沈阳药科大学基于靶点的药物设计与研究教育部重点实验室;
【基金】：国家“重大新药创制”科技重大专项(2009ZX09301-012)
【分类号】：R914.5
，
本文编号：2332613
[Abstract]:Objective to synthesize the impurity A of citaletine. Methods the intermediate 1- {3- trifluoromethyl-56-dihydro-1H _ 1H _ 2H _ 2H _ 3H _ 3H _ 3H _ 3H _ 2H _ 3H _ 2H _ 2H _ 2H _ 2H _ 2H _ 2H _ 2H _ 1H _ 1H _ 1H _ 2 was obtained by one-pot reaction. 4-triazolo-7 (8H) -yl} -4- (2o 4N 5- trifluorophenyl) -1H 3-butanedione was reduced by sodium borohydride to obtain the impurity A. Results the structure of the target compound was confirmed by IR,MS and 1H-NMR. Conclusion the method has the advantages of low cost, simple operation, mild reaction and high yield.
【作者单位】： 沈阳药科大学基于靶点的药物设计与研究教育部重点实验室;
【基金】：国家“重大新药创制”科技重大专项(2009ZX09301-012)
【分类号】：R914.5
，
本文编号：2332613
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