Direct Electrophilic Acylation of N-Substituted Pyrazoles by Anhydrides of Carboxylic Acids

Ilya V. Taydakov; Sergey S. Krasnoselskiy

doi:10.1055/s-0033-1338923

Synthesis, Inhaltsverzeichnis

Synthesis 2013; 45(15): 2188-2192
DOI: 10.1055/s-0033-1338923

paper

Direct Electrophilic Acylation of N-Substituted Pyrazoles by Anhydrides of Carboxylic Acids

Authors

Ilya V. Taydakov*

^aP.N. Lebedev Physical Institute of the Russian Academy of Sciences, Leninskiy prospect 53, 119991 Moscow, Russian Federation Fax: +7(495)6000603 eMail: taidakov@gmail.com
Sergey S. Krasnoselskiy

^bPeople’s Friendship University of Russia, Miklukho-Maklaya str. 6, 117198 Moscow, Russian Federation

Abstract

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Abstract

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.

Key words

electrophilic aromatic acylation - heterocycles - ketones - catalysis

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Referenzen

References

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