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Synthesis 2015; 47(02): 235-241
DOI: 10.1055/s-0034-1379474
DOI: 10.1055/s-0034-1379474
paper
A Convenient and Practical Synthesis of Aminopyrazoles
Weitere Informationen
Publikationsverlauf
Received: 28. Juli 2014
Accepted after revision: 21. September 2014
Publikationsdatum:
11. November 2014 (online)
This manuscript is dedicated to Dr. John A. Myers on the occasion of his retirement from NCCU Chemistry.
Abstract
A selective methodology for preparing highly substituted aminopyrazoles has been demonstrated. Starting with an acetophenol core, the corresponding substituted isoxazole is prepared in two steps. The isoxazole is transformed into a benzopyran. Alkylation of the aminobenzopyranone gives N-substituted aminobenzopyranone derivatives that react with substituted hydrazine to give aminopyrazoles. This versatile synthesis enables the preparation of highly substituted aminopyrazoles for use as key synthetic building blocks for biologically active molecules. In addition, this process represents the first amine alkylation of aminobenzopyranones.
Supporting Information
- Supporting information for this article is available online at http://dx.doi.org/10.1055/s-0034-1379474.
- Supporting Information
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