Issue 29, 2020
From the journal:

Organic & Biomolecular Chemistry

Pyrazoles: ‘one-pot’ synthesis from arenes and carboxylic acids†

Jung Keun Kim, ORCID logo ‡ab   Ming Gong,‡b   Elvira A. Shokova,a   Viktor A. Tafeenko,a   Olga V. Kovaleva,c   Yangjie Wu ORCID logo *b  and  Vladimir V. Kovalev ORCID logo *a  

* Corresponding authors

a Department of Chemistry, Moscow State University, Lenin's Hills, Moscow 119991, Russia
E-mail: kovalev@petrol.chem.msu.ru

b College of Chemistry, Henan Key Laboratory of Chemical Biology and Organic Chemistry, Key Laboratory of Applied Chemistry of Henan Universities, Zhengzhou University, Zhengzhou 450052, P.R. China
E-mail: wyj@zzu.edu.cn

c Institute of Carcinogeneis, NN Blokhin Russian Cancer Research Center, Moscow 115478, Russia

Abstract

A rapid and efficient method for ‘one-pot’ synthesis of pyrazoles from (hetero)arenes and carboxylic acids via successive formation of ketones and β-diketones followed by heterocyclization with hydrazine has been developed. The utility of the RCOOH/TfOH/TFAA acylation system for intermediate production of ketones and 1,3-diketones is a key feature of this approach. The preliminary evaluation of the anticancer activity of the synthesized pyrazoles is performed.

Graphical abstract: Pyrazoles: ‘one-pot’ synthesis from arenes and carboxylic acids

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Article information

DOI
https://doi.org/10.1039/D0OB01228A
Article type
Paper
Submitted
15 Jun 2020
Accepted
29 Jun 2020
First published
30 Jun 2020

Org. Biomol. Chem., 2020,18, 5625-5638

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Pyrazoles: ‘one-pot’ synthesis from arenes and carboxylic acids

J. K. Kim, M. Gong, E. A. Shokova, V. A. Tafeenko, O. V. Kovaleva, Y. Wu and V. V. Kovalev, Org. Biomol. Chem., 2020, 18, 5625 DOI: 10.1039/D0OB01228A

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