【摘要】：目的合成西他列汀雜質(zhì)A。方法將2,4,5-三氟苯乙酸、米氏酸和3-三氟甲基-5,6,7,8-四氫-1,2,4-三唑[4,3-α]吡嗪鹽酸鹽以"一鍋法"反應(yīng)得到中間體1-{3-三氟甲基-5,6-二氫-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,再經(jīng)硼氫化鈉還原得到西他列汀雜質(zhì)A。結(jié)果目標化合物的結(jié)構(gòu)經(jīng)IR、MS和1H-NMR確證。結(jié)論該方法未見文獻報道,具有成本低、操作簡單、反應(yīng)溫和、收率高等優(yōu)點。
[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.
【作者單位】： 沈陽藥科大學(xué)基于靶點的藥物設(shè)計與研究教育部重點實驗室;
【基金】：國家“重大新藥創(chuàng)制”科技重大專項(2009ZX09301-012)
【分類號】：R914.5
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本文編號：2332613