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Issue 18, 2010
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Microwave-enhanced synthesis of 2,3,6-trisubstituted pyridazines: application to four-step synthesis of gabazine (SR-95531)

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Abstract

Microwave-enhanced, highly efficient protocols for the synthesis of synthetically and biologically important 2,3,6-trisubstituted pyridazine architectures have been developed by sequential amination/Suzuki coupling/alkylation reactions. This powerful strategy is an economical and highly chemoselective protocol for the synthesis of diversified pyridazines. The total synthesis of gabazine (SR-95531) has been achieved using a versatile strategy in four steps and 73% overall yield.

Graphical abstract: Microwave-enhanced synthesis of 2,3,6-trisubstituted pyridazines: application to four-step synthesis of gabazine (SR-95531)

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Supplementary files

Article information


Submitted
15 Apr 2010
Accepted
17 Jun 2010
First published
26 Jul 2010

Org. Biomol. Chem., 2010,8, 4131-4136
Article type
Paper

Microwave-enhanced synthesis of 2,3,6-trisubstituted pyridazines: application to four-step synthesis of gabazine (SR-95531)

N. Gavande, G. A. R. Johnston, J. R. Hanrahan and M. Chebib, Org. Biomol. Chem., 2010, 8, 4131
DOI: 10.1039/C0OB00004C

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