Synthesis 2013; 45(15): 2188-2192
DOI: 10.1055/s-0033-1338923
paper
© Georg Thieme Verlag Stuttgart · New York

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

Ilya V. Taydakov*
a  P.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
b  People’s Friendship University of Russia, Miklukho-Maklaya str. 6, 117198 Moscow, Russian Federation
› Author Affiliations
Further Information

Publication History

Received: 10 March 2013

Accepted after revision: 30 April 2013

Publication Date:
12 June 2013 (online)


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.

 
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