Preparation of highly functionalized 1,5-disubstituted tetrazoles via palladium-catalyzed Suzuki coupling |
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Authors: | Edward J Hennessy Mark Cornebise Lakshmaiah Gingipalli Tyler Grebe Sudhir Hande Valerie Hoesch Hoan Huynh Scott Throner Jeffrey Varnes Ye Wu |
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Institution: | IMED Oncology, Innovative Medicines & Early Development, AstraZeneca, 35 Gatehouse Drive, Waltham, MA 02451, United States |
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Abstract: | The preparation of a range of 1,5-disubstituted tetrazoles has been achieved through palladium-catalyzed Suzuki coupling. Using appropriately substituted 5-p-toluenesulfonyltetrazoles as substrates (obtained by cycloaddition of a substituted azide with p-toluenesulfonyl cyanide), this methodology provides access to a variety of highly substituted tetrazoles that would be difficult to access otherwise. The procedure is compatible with functional groups commonly found in drug-like molecules, and has been used to generate a number of compounds of potential biological interest. |
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Keywords: | Tetrazoles Heterocycles Suzuki coupling Biologically-active Molecules |
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