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5-Aryltetrazoles from Direct C-H Arylation with Aryl Bromides

Yuan Zhang*, Jack Chang Hung Lee, Matthew R. Reese, Brian P. Boscoe, John M. Humphrey and Christopher J. Helal

*Pfizer Worldwide Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States, Email:

Y. Zhang, J. C. H. Lee, M. R. Reese, B. P. Boscoe, J. N. Humphrey, C. H. Helal, J. Org. Chem., 2020, 85, 5718-5723.

DOI: 10.1021/acs.joc.0c00085

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A Pd/Cu cocatalytic system enables a mild, direct C-H arylation of 1-substituted tetrazoles with readily available aryl bromides to 5-aryltetrazoles. The methodology tolerates a wide range of functionalities and avoids late-stage usage of azides.

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Key Words


ID: J42-Y2020