Regioselective Palladium-Catalyzed Arylation of 4-Chloropyrazoles
- 7 October 2010
- journal article
- Published by American Chemical Society (ACS) in Organic Letters
- Vol. 12 (21), 4924-4927
- https://doi.org/10.1021/ol1020898
Abstract
A highly regioselective Pd-catalyzed arylation of N-methylpyrazoles with aryl bromides is described. This transformation was studied extensively via automated reaction screening. A Design of Experiments (DoE) approach for optimizing the critical parameters was applied, resulting in excellent conditions for preparing selectively 5-arylpyrazoles in moderate to excellent yields under mild conditions.Keywords
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