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Synfacts 2007(8): 0803-0803
DOI: 10.1055/s-2007-968800
DOI: 10.1055/s-2007-968800
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart · New York
Direct Pd-Catalyzed Arylation of Triazoles
S. Chuprakov, N. Chernyak, A. S. Dudnik, V. Gevorgyan*
University of Illinois at Chicago, USA
Further Information
Publication History
Publication Date:
24 July 2007 (online)

Significance
Reported here is a development of a highly efficient method for the synthesis of 5-aryl 1,2,3-triazoles via a direct Pd-catalyzed C-H coupling with aryl bromides. Introduction of both electron-rich and -deficient aryl groups was successfully executed. Similarly, regioselective C-5 arylation of N-substituted 1,2,3-triazoles with aryl bromides bearing EWGs and EDGs was efficiently achieved. On the other hand, in a limited study C-4 arylation of 1,5-disubstituted 1,2,3-triazoles was found to be very sluggish and produced only moderate yields.