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<p>The regioselectivity of the cyclization of 7-[(<i>E</i>)-2-(dimethylamino)vinyl]pyrazolo-[1,5-<i>a</i>]pyrimidine-6-carbonitriles was studied in the reactions with hydrazine hydrate. Depending on the conditions, the reaction in acetic acid or DMF affords either linear 6-(1<i>H</i>-pyrazol-5-yl)pyrazolo[1,5-<i>a</i>]pyrimidin-7-amines <i>via</i> the ANRORC rearrangement or fused 6-iminopyrazolo[1,5-<i>a</i>]pyrido[3,4-<i>e</i>]pyrimidin-7(6<i>H</i>)-amines. The preliminary <i>in vitro</i> screening of the antibacterial activity of the synthesized compounds was performed against <i>E. coli</i> and <i>S. aureus</i>.</p>

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Reaction of 7-[(E)-2-(dimethylamino)vinyl]pyrazolo[1,5-a]pyrimidine-6-carbonitriles with hydrazine hydrate and preliminary studies of antimicrobial properties of reaction products

  • 期刊论文

  • 发表日期：

    2025年10月1日

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  • V. A. Polikarchuk,
  • M. G. Holyavka,
  • Kh. S. Shikhaliev

摘要

The regioselectivity of the cyclization of 7-[(E)-2-(dimethylamino)vinyl]pyrazolo-[1,5-a]pyrimidine-6-carbonitriles was studied in the reactions with hydrazine hydrate. Depending on the conditions, the reaction in acetic acid or DMF affords either linear 6-(1H-pyrazol-5-yl)pyrazolo[1,5-a]pyrimidin-7-amines via the ANRORC rearrangement or fused 6-iminopyrazolo[1,5-a]pyrido[3,4-e]pyrimidin-7(6H)-amines. The preliminary in vitro screening of the antibacterial activity of the synthesized compounds was performed against E. coli and S. aureus.