摘要/Abstract

吡唑并嘧啶酮类化合物由于其与生物体内嘌呤的结构相似而具有多种活性, 进而被广泛研究和应用. 吡唑并嘧啶酮类化合物传统的合成方法存在一些不足, 如需要酰化、环化两步完成等. 报道了一种以水为介质、氢氧化钠作用下的5-氨基-4-氰基吡唑和芳香醛一锅环合形成1H-吡唑并[3,4-d]嘧啶-4(5H)-酮的方法. 该方法具有原料易得、操作简单、良好的底物耐受性等优点.
关键词: 一锅转化, 吡唑并[3,4-d]嘧啶-4(5H)-酮, 氢氧化钠, 绿色溶剂, 水
Abstract Pyrazolopyrimidinone compounds have many biological activities and been widely used due to the similar structure of purines in organisms. However, the traditional synthetic methods suffered from several drawbacks, such as acylation and cyclization. Herein, one pot cyclization of 1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one was developed by one pot conversion of 5-amino-4-cyano-pyrazole and aromatic aldehydes in the presence of sodium hydroxide using water as media. The reaction was carried out under the conditions of easily available raw materials, simple operation, and showed good tolerance to various functional groups.
Key words: one pot conversion, pyrazolo[3,4-d]pyrimidin-4(5H)-one, sodium hydroxide, green solvent, water


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