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<p></p><p>A reliable systematic approach to a series of substituted 4-(pyrrolidin-2-ylidene)pyrazol-5-ones was developed. The compounds were synthesized through the reaction of pyrazol-5-ones with cyclic lactim ethers or lactam acetals. Subsequent treatment with phosphorus oxychloride yielded 5-chloro-4-(3,4-dihydro-2<i>H</i>-pyrrol-5-yl)-1<i>H</i>-pyrazoles, which possess both an active chlorine atom and an imine group. These intermediates underwent stepwise reduction – either targeting the imine group followed by reductive dechlorination, or <i>vice versa</i> – a direct reduction to produce 4-(pyrrolidin-2-yl)pyrazoles. These products serve as valuable building blocks in medicinal chemistry, offering potential for further functionalization and application in drug design.</p>

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Various approaches to 4-(pyrrolidin-2-yl)pyrazoles

  • 期刊论文

  • 发表日期：

    2026年5月13日

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  • Tetiana I. Shvydenko,
  • Viacheslav A. Lysenko,
  • Sergiy L. Filimonchuk,
  • Svitlana V. Shishkina,
  • Kostiantyn G. Nazarenko,
  • Aleksandr N. Kostyuk

摘要

A reliable systematic approach to a series of substituted 4-(pyrrolidin-2-ylidene)pyrazol-5-ones was developed. The compounds were synthesized through the reaction of pyrazol-5-ones with cyclic lactim ethers or lactam acetals. Subsequent treatment with phosphorus oxychloride yielded 5-chloro-4-(3,4-dihydro-2H-pyrrol-5-yl)-1H-pyrazoles, which possess both an active chlorine atom and an imine group. These intermediates underwent stepwise reduction – either targeting the imine group followed by reductive dechlorination, or vice versa – a direct reduction to produce 4-(pyrrolidin-2-yl)pyrazoles. These products serve as valuable building blocks in medicinal chemistry, offering potential for further functionalization and application in drug design.