271-34-1Relevant articles and documents
A medicine intermediate 5 - aza indole synthesis method (by machine translation)
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, (2019/03/28)
The present invention discloses a pharmaceutical intermediate 5 - aza indole synthesis method, comprises the following steps: the 3 - methyl - 4 - aminopyridine with acetone after mixing, heating to 40 - 60 °C, adding catalyst after adding the oxalate, under stirring conditions, refluxing reaction 1 - 2 h, filtering, the filtrate by reduced pressure distillation, recrystallization, prepared 4 - aminopyridine - 3 - pyruvate ester; in its entry into the DMA, adding salicylic acid then adding the FeO, heated to 60 - 70 °C, stirring reflux reaction for 2 - 3 h, filter, the filtrate is distilled under reduced pressure, to obtain 5 - aza indole - 2 - carboxylic acid; and after mixing with the carbon tetrachloride, heating to 70 - 90 °C, adding ZnO mixing, stirring reflux reaction for 2 - 3 h after, filtering, the filtrate is distilled under reduced pressure, to obtain 5 - azaindole. The application of the synthesis method is simple in operation, mild condition, less by-products, the product has high purity, product yield is relatively high. (by machine translation)
Preparation method of5-diazaindene
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Paragraph 0016; 0017; 0018; 0019; 0020; 0021-0039, (2017/04/26)
The invention discloses apreparation method of 5-diazaindene. 3-methyl-4-aminopyridine is evenly stirred and mixed with acetic anhydride and a catalyst for reaction, the obtained product is evenly mixed with pyrrolidine and DMF-DMA, reaction is performed at the temperature of 80-90 DEG Cunder the condition of the catalyst for 2-3 hours to obtain the final product 5-diazaindene. The method produces fewer by-products and is high in productpurity.In addition, the added novel catalyst makes reaction temperaturemore moderate, and reaction time is shortened greatly. In a word, the steps of the whole production process are simple, operation is easy, the cost of large-scale industrial production is low, and implementation is easy.
Design, synthesis and antiproliferative activity evaluation of new 5-azaisoindigo derivatives
Zhao, Ping,Yan, Yun,Li, Yanzhong,Zhang, Aiying,Zhan, Xiaoping,Liu, Zenglu,Mao, Zhenmin,Chen, Shaoxiong,Wang, Liqun
, p. 1923 - 1932 (2014/08/18)
New 5-azaisoindigo derivatives were synthesized with two key intermediates 5-azaoxindole (7) and substituted indole-2,3-dione (10) in this paper. Intermediate 7 was prepared from 3-methylpyridine (1) through 6 steps containing oxidation reaction and so on. Intermediate 10 was obtained by a convenient Sandmeyer's method. The target compounds 5-azaisoindigo derivatives 11a-f were obtained by condensation of these two intermediates 7 and 10 in acidic condition. All target compounds were evaluated for their antiproliferative activity against seven cell lines by SRB assay. Compounds 11e and 11f showed significant antiproliferative activity against K562 cells (IC50: 8.9 μM and 13.6 μM, respectively).