Direct Electrophilic Acylation of N-Substituted Pyrazoles by Anhydrides of Carboxylic Acids
Direct Electrophilic Acylation of N-Substituted Pyrazoles by Anhydrides of Carboxylic Acids
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DOI：
10.1055/s-0033-1338923
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发表时间：
2013-06
期刊：
影响因子：
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通讯作者：
I. Taydakov;S. S. Krasnoselskiy-S.
中科院分区：
文献类型：
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作者：
I. Taydakov;S. S. Krasnoselskiy-S.
本文介绍了一种简便、可放大的1-取代-4-酰基吡唑的合成方法，即在浓硫酸催化下，吡唑与脂肪族、芳香族和氟代羧酸的酸酐直接酰化反应。以41-86%的分离产率获得高纯度的目标酮，而无需费力的纯化。讨论了该方法的范围和局限性。
A simple, convenient and scalable approach to 1-substituted 4-acylpyrazoles through direct acylation of pyrazoles by anhydrides of aliphatic, aromatic and fluorinated carboxylic acids in the presence of concentrated sulfuric acid as a catalyst is described. Target ketones were obtained in 41–86% isolated yields in high purity without laborious purification. The scope and limitations of the method are discussed.