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Rapid Synthesis of 1,3,5-Substituted 1,2,4-Triazoles from Carboxylic Acids, Amidines, and Hydrazines

Georgette M. Castanedo*, Pamela S. Seng, Nicole Blaquiere, Sean Trapp and Steven T. Staben*

*Discovery Chemistry Group, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States, Email:,

G. M. Castanedo, P. S. Seng, N. Blaquiere, S. Trapp, S. T. Staben, J. Org. Chem., 2011, 76, 1177-1179.

DOI: 10.1021/jo1023393


A highly regioselective one-pot process provides rapid access to highly diverse 1,3,5-trisubstituted 1,2,4-triazoles from reaction of carboxylic acids, primary amidines, and monosubstituted hydrazines.

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ID: J42-Y2010-0370