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Synthesis 2013; 45(6): 830-836
DOI: 10.1055/s-0032-1316856
DOI: 10.1055/s-0032-1316856
paper
Facile One-Pot Synthesis of 3,5-Disubstituted 1H-Pyrazoles from Propargylic Alcohols via Propargyl Hydrazides
Further Information
Publication History
Received: 17 December 2012
Accepted after revision: 25 January 2013
Publication Date:
08 February 2013 (online)
Abstract
A new and efficient metal-free, two-component, one-pot approach to a variety of 3,5-disubstituted 1H-pyrazoles has been developed from propargylic alcohols. This transformation proceeds via an acid-catalyzed propargylation of N,N-diprotected hydrazines followed by base-mediated 5-endo-dig cyclization leading to 3,5-disubstituted 1H-pyrazoles in good overall yields.
Supporting Information
- for this article is available online at http://www.thieme-connect.com/ejournals/toc/synthesis.
- Supporting Information
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